International Journal of Advances in Pharmaceutics
International Journal of Advances in Pharmaceutics (IJAP) is a bi-monthly publication committed to publishing online the original scientific research and reviews in the field of Pharmaceutical Sciences. It mainly covers the articles of special interest, covering the areas of Pharmaceutical research, recent technology & discoveries in the emerging arena of Pharmaceutics and pharmaceutical technology. ISSN: 2320-4931 (Online); 2320-4923 (Print)
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Design, Development and characterization of fast dissolving oral films for rapid delivery of Loratadine
Fast dissolving oral films (FDOFs) represent an innovative drug delivery system that disintegrates rapidly in the oral cavity without water, enhancing patient compliance and therapeutic onset. Loratadine, a second‑generation antihistamine for allergic rhinitis and chronic urticaria, suffers from poor aqueous solubility, limiting dissolution and onset of action. Developing FDOFs of Loratadine offers a promising approach to improve drug release and acceptability. The present study aimed to design, develop, and characterize Loratadine FDOFs using the solvent casting technique. Hydroxypropyl methylcellulose (HPMC E15 and HPMC E5) served as film‑forming polymers, with polyethylene glycol 400, glycerin, and propylene glycol as plasticizers. Tween 80 was incorporated as a surfactant, while citric acid and sodium saccharin acted as saliva‑stimulating agent and sweetener, respectively. Prepared films were evaluated for physical appearance, thickness, weight variation, folding endurance, surface pH, tensile strength, drug content, disintegration time, in vitro drug release, and stability under ICH guidelines. All formulations yielded smooth, flexible, uniform films with satisfactory mechanical properties. Among them, formulation F3 demonstrated optimal performance, showing uniform drug content, excellent folding endurance, rapid disintegration, and highest cumulative drug release. Accelerated stability studies at 40 ± 2°C/75 ± 5% RH for 90 days revealed no significant changes in physicochemical properties, confirming good stability. In conclusion, the optimized Loratadine FDOF exhibited rapid disintegration, efficient drug release, satisfactory mechanical strength, and excellent stability. This formulation represents a promising alternative to conventional oral dosage forms, with potential to improve patient compliance and provide rapid therapeutic action in allergic disorders.
Copyright (c) 2026 International Journal of Advances in Pharmaceutics https://creativecommons.org/licenses/by/4.0
Development and evaluation of enteric coated tablet of Esomeprazole
Esomeprazole5-methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]-1H-benzimidazole is a proton pump inhibitor belongs to group of benzimidazole . This compound inhabits gastric acid formation and thereby it is very efficient for the treatment of gastric and duodenum ulcers. In aqueous media more acidic than pH 4 it suffers a practically complete decomposition within a period shorter than 10 minutes. Even in solid state it is sensitive to heat, humidity, and light and especially to substances containing an acidic group. Esomeprazole which has an irritant effect on the stomach can be coated with a substance that will only dissolve in the small intestine. For such types of drugs, enteric coating added to the formulation tends to avoid the stomach's acidic exposure, delivering them instead to a basic pH environment (intestines pH 5.5 and above) where they do not degrade, and give their desired action. This stimulates us to formulate and evaluate esomeprazole as a enteric coated tablet.
Formulation and evaluation of Famotidine-loaded ethosomal vesicles for ulcer therapy
Background: Famotidine, an H₂‑receptor antagonist, suffers from variable bioavailability and frequent dosing requirements. Ethosomes, lipid‑based nanocarriers, offer improved encapsulation, stability, and sustained release. Objective: To formulate, optimize, and characterize Famotidine‑loaded ethosomes, assessing physicochemical properties, entrapment efficiency, release behavior, kinetics, and stability. Methods: Famotidine-loaded ethosomes were prepared using the ethanol injection method by varying the concentrations of soya lecithin and ethanol. Prior to formulation, the drug was characterized through organoleptic evaluation, solubility analysis, melting point determination, partition coefficient measurement, UV-visible spectrophotometric analysis, and Fourier-transform infrared (FTIR) spectroscopy. The prepared formulations (F1–F5) were evaluated for particle size, polydispersity index, zeta potential, scanning electron microscopy (SEM), entrapment efficiency, in vitro drug release using the dialysis bag diffusion method, release kinetics, and accelerated stability studies under ICH-recommended storage conditions. Results: Preformulation studies confirmed the identity and purity of Famotidine, with a melting point of 154°C, λmax at 294 nm, and a partition coefficient of 2.16. FTIR analysis demonstrated the preservation of the characteristic functional groups, indicating the absence of significant chemical interactions during formulation. Among the five formulations, F4 exhibited the most desirable characteristics, with the smallest particle size (149.1 nm), zeta potential of −12.1 mV, and the highest entrapment efficiency (89.63%). SEM analysis revealed uniformly distributed, spherical vesicles with smooth surface morphology. The optimized formulation achieved 96.83% cumulative drug release within 14 h, demonstrating sustained release behaviour. Drug release followed the Higuchi diffusion model (R² = 0.979),indicating diffusion-controlled release from the vesicular matrix. Accelerated stability studies conducted for 90 days showed negligible changes in particle size and entrapment efficiency, confirming the physicochemical stability of the optimized ethosomal formulation. Conclusion: Optimized Famotidine ethosomes showed high entrapment, sustained release, and excellent stability. Ethosomal nanovesicles are promising carriers to enhance Famotidine’s performance. Further in vivo studies are needed to confirm clinical potential.
Assessment of the Compatibility of Famotidine with Selected Pharmaceutical Excipients
A drug–excipient compatibility study was performed to investigate the stability of Famotidine in combination with Polyvinylpyrrolidone (PVP K30), Polyethylene Glycol (PEG 6000), and Hydroxypropyl Methylcellulose (HPMC) under accelerated storage conditions. Physical mixtures of Famotidine and excipients were stored at 40°C/75% Relative Humidity (RH) and 50 ± 2°C for an appropriate duration (typically 30–90 days) and evaluated for possible physical and chemical interactions. The compatibility studies conducted under accelerated conditions of 40°C/75% RH and 50 ± 2°C demonstrated that Famotidine is compatible with PVP K30, PEG 6000, and HPMC. No significant physical changes, chemical degradation, or drug–excipient interactions were observed during storage. The characteristic thermal and spectroscopic properties of Famotidine were retained throughout the study period. Therefore, PVP K30, PEG 6000, and HPMC are considered suitable excipients for the formulation development of Famotidine, particularly in solid dispersions, tablets, and other solid dosage forms requiring enhanced solubility and stability.
Mucoadhesive buccal films: A promising approach for Controlled Drug Delivery
Mucoadhesive buccal films have emerged as an advanced and patient-friendly controlled drug delivery system for both local and systemic therapy. These films are designed to adhere to the buccal mucosa and release the drug in a controlled manner, thereby improving therapeutic efficacy and patient compliance. Buccal drug delivery offers several advantages including avoidance of hepatic first-pass metabolism, protection from gastrointestinal degradation, rapid onset of action, and improved bioavailability. Due to these advantages, buccal films are increasingly explored for the delivery of various drugs, particularly those with poor oral bioavailability. Mucoadhesive buccal films are commonly prepared using natural and synthetic polymers such as Hydroxypropyl Methylcellulose (HPMC), Carbopol, Polyvinyl Alcohol (PVA), and Chitosan. Among various preparation methods, solvent casting technique is the most widely employed because of its simplicity and ability to produce uniform films. Evaluation parameters including thickness, folding endurance, tensile strength, swelling index, mucoadhesive strength, drug content, and in-vitro drug release are important for optimization of film performance. Recent advances in buccal film technology include the incorporation of nanoparticles, permeation enhancers, bilayer systems, and smart polymers to improve drug permeation and controlled release behavior. Buccal films have demonstrated promising applications in the delivery of antidiabetic, antihypertensive, analgesic, antimicrobial, and peptide drugs. This review highlights the anatomy of buccal mucosa, mechanism of mucoadhesion, polymers used in buccal films, methods of preparation, evaluation parameters, advantages, limitations, recent advances, and future prospects of mucoadhesive buccal films as a promising approach for controlled drug delivery.
Formulation and Evaluation of Mucoadhesive Buccal Films of Glimepiride Using HPMC–Carbopol Polymer Blend for Enhanced Drug Release and Patient Compliance
The present study aimed to formulate and evaluate mucoadhesive buccal films of Glimepiride using a polymer blend of Hydroxypropyl Methylcellulose (HPMC K15M) and Carbopol 934P for enhanced drug release and improved patient compliance. Glimepiride, a third-generation sulfonylurea antidiabetic drug, exhibits limitations such as poor aqueous solubility and first-pass metabolism, which may reduce its therapeutic effectiveness following conventional oral administration. Buccal drug delivery was selected as an alternative route to bypass hepatic first-pass metabolism and improve systemic bioavailability. Mucoadhesive buccal films were prepared by solvent casting technique using HPMC K15M, Carbopol 934P, Polyvinyl Alcohol (PVA), and Chitosan. Prepared formulations were evaluated for physicochemical properties including thickness, weight variation, folding endurance, surface pH, drug content, tensile strength, percentage elongation, mucoadhesive strength, swelling index, and in-vitro drug release. Drug–excipient compatibility studies were performed using Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC). Ex-vivo permeation studies were conducted using goat buccal mucosa and Franz diffusion cell. Stability studies were carried out under accelerated conditions according to ICH guidelines. Among all formulations, formulation F6 exhibited optimum physicochemical and mechanical properties, high mucoadhesive strength, controlled swelling behavior, and sustained drug release profile. Drug release kinetics followed the Korsmeyer–Peppas model, indicating a non-Fickian diffusion mechanism. Stability studies confirmed the stability of the optimized formulation under accelerated storage conditions.The study concluded that mucoadhesive buccal films of Glimepiride prepared using HPMC–Carbopol polymer blend offer a promising alternative to conventional oral dosage forms by improving drug release characteristics, reducing dosing frequency, and enhancing patient compliance.
Formulation, development, and evaluation of chitosan mucoadhesive microspheres of Atenolol, a selective beta blocker
Atenolol, a selective β₁-adrenergic blocker, requires chronic administration for hypertension and related cardiovascular disorders. Conventional oral dosage forms may lead to plasma peak–trough fluctuations and frequent dosing. The present work aimed to develop chitosan-based mucoadhesive microspheres of atenolol to achieve prolonged gastrointestinal residence and sustained drug release. Microspheres were prepared using ionotropic gelation with sodium tripolyphosphate (TPP) as a cross-linking agent. Formulations (F1–F6) were optimized by varying polymer and cross-linker levels. Prepared microspheres were evaluated for percentage yield, particle size, drug loading, entrapment efficiency, flow properties, swelling index, mucoadhesive strength, in-vitro wash-off, surface morphology (SEM), in-vitro drug release, and release kinetics. Microspheres were discrete and spherical, showing acceptable flow and significant mucoadhesion. The optimized formulation (F2) exhibited high yield, satisfactory entrapment, strong mucoadhesion, and sustained release up to 12 h. Release kinetics indicated diffusion-dominant release with swelling contribution, consistent with Higuchi and Korsmeyer–Peppas behavior. The study concludes that chitosan mucoadhesive microspheres represent a promising controlled oral delivery platform for atenolol.
Optimization and evaluation of fast dissolving oral films of Venlafaxine Hydrochloride
Fast dissolving oral films (FDOFs) have emerged as a promising patient-centric drug delivery system designed to overcome the limitations associated with conventional oral solid dosage forms, such as swallowing difficulty, delayed onset of action, and poor patient compliance. The present research work was aimed at the optimization and evaluation of fast dissolving oral films of Venlafaxine Hydrochloride, a serotonin–norepinephrine reuptake inhibitor widely used in the management of depressive and anxiety disorders. Fast dissolving oral films were prepared using the solvent casting method with hydrophilic film-forming polymers and suitable plasticizers. The prepared films were evaluated for physicomechanical properties including thickness, weight uniformity, folding endurance, tensile strength, surface pH, disintegration time, drug content uniformity, and in-vitro drug release. Optimization was carried out by varying polymer and plasticizer concentrations to achieve rapid disintegration and adequate mechanical strength. The optimized formulation demonstrated uniform drug distribution, satisfactory mechanical properties, rapid disintegration within seconds, and more than 95% drug release within a short duration, indicating fast availability of the drug. Stability studies conducted under accelerated conditions showed no significant changes in physical appearance, drug content, or dissolution behavior, confirming formulation stability. The study concludes that fast dissolving oral films of Venlafaxine Hydrochloride represent a safe, effective, and patient-friendly alternative to conventional oral dosage forms, with potential to enhance therapeutic efficacy, patient compliance, and quality of life.
Formulation development and evaluation of immediate release of Esmolol Hydrochloride tablet of antihypertensive drug
Esmolol hydrochloride is a cardioselective β₁-adrenergic blocker widely used for the rapid management of hypertension and tachyarrhythmias. The present study was undertaken to develop and evaluate an immediate-release (IR) tablet formulation of esmolol hydrochloride using the direct compression technique, with the objective of achieving rapid drug release and acceptable tablet characteristics. Preformulation studies were carried out to assess physicochemical properties, flow behavior, and drug–excipient compatibility. Several tablet formulations (F1–F6) were prepared using different concentrations of superdisintegrants such as croscarmellose sodium and sodium starch glycolate along with suitable diluents and lubricants. The prepared powder blends were evaluated for flow properties, while compressed tablets were assessed for weight variation, hardness, thickness, friability, disintegration time, drug content uniformity, and in vitro dissolution. All formulations complied with pharmacopoeial requirements for physical parameters. In vitro dissolution studies demonstrated rapid drug release, with the optimized formulation releasing more than 85% of esmolol hydrochloride within 30 minutes. The study concludes that an optimized immediate-release tablet of esmolol hydrochloride can be successfully developed using appropriate superdisintegrants, providing rapid drug release and consistent tablet quality, suitable for further stability and scale-up studies.
Development and evaluation of enteric-coated tablets: A review
Enteric-coated tablets represent an important category of modified oral drug delivery systems designed to prevent drug release in the acidic environment of the stomach and allow selective release in the intestine. This dosage form is particularly beneficial for drugs that are unstable in gastric conditions, cause gastric irritation, or require site-specific intestinal absorption. The development of enteric-coated tablets involves careful selection of core tablet composition, enteric polymers, coating techniques, and evaluation methods to ensure consistent performance and regulatory compliance. Various polymers, including cellulose-based derivatives and methacrylic acid copolymers, have been extensively studied for their pH-dependent solubility and film-forming properties. Evaluation of enteric-coated tablets includes tests for acid resistance, disintegration, dissolution, stability, and release kinetics. This review provides a comprehensive overview of the principles, formulation strategies, coating technologies, polymers used, and evaluation parameters involved in the development of enteric-coated tablets, highlighting their significance in improving therapeutic efficacy, gastric tolerability, and patient compliance.
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Formulation, development, and evaluation of orally disintegrating tablets of Atenolol
Orally disintegrating tablets (ODTs) have emerged as a patient-friendly dosage form designed to improve compliance, especially in pediatric, geriatric, and dysphagic patients. Atenolol, a β₁-selective adrenergic blocker widely prescribed for hypertension, requires long-term administration and is therefore an ideal candidate for ODT formulation. The present study aimed to develop and optimize Atenolol ODTs using the direct compression method. Nine formulations (F1–F9) were prepared employing different superdisintegrants—crospovidone, croscarmellose sodium, and sodium starch glycolate—at varying concentrations. Preformulation studies confirmed drug purity, solubility, and compatibility with excipients. Prepared blends were evaluated for pre-compression parameters, while compressed tablets were assessed for post-compression characteristics, special ODT tests, in-vitro disintegration, dissolution behavior, and stability. All formulations complied with pharmacopeial limits. Among them, formulation F2 containing crospovidone exhibited the shortest disintegration time (~16 s) and maximum drug release (~99.8% within 30 min). Statistical analysis using one-way ANOVA demonstrated significant differences among formulations (p < 0.05). Accelerated stability studies confirmed formulation stability. The study concludes that Atenolol can be successfully formulated as an ODT with rapid disintegration, fast drug release, and acceptable mechanical strength, offering a promising alternative to conventional tablets.
Design, development, and evaluation of enteric coated tablets of Ciprofloxacin using different polymers
Ciprofloxacin is a broad-spectrum fluoroquinolone antibiotic widely used for the treatment of bacterial infections; however, its conventional oral dosage forms are often associated with gastric irritation and non-targeted drug release in the stomach. The present study aimed to design, develop, and evaluate enteric coated tablet formulations of Ciprofloxacin to achieve gastric protection and targeted intestinal drug release. Core tablets were prepared by the wet granulation method and subsequently coated with different pH-dependent enteric polymers. Preformulation studies confirmed the identity, purity, and compatibility of Ciprofloxacin with selected excipients. Core tablets were evaluated for micromeritic and post-compression parameters, while enteric coated tablets were assessed for acid resistance, disintegration behavior, and in-vitro dissolution. All enteric coated formulations exhibited complete resistance in acidic medium and rapid drug release in phosphate buffer pH 6.8. Among the tested polymers, methacrylic acid copolymer–based coatings showed superior performance with faster intestinal disintegration and higher drug release. Accelerated stability studies demonstrated good stability of the optimized formulation. The study concludes that enteric coating is an effective strategy to improve the oral delivery of Ciprofloxacin by minimizing gastric exposure and ensuring targeted intestinal release.
Design, development, and formulation of Glipizide fast-dissolving tablets
Fast-dissolving tablets (FDTs) are designed to disintegrate rapidly in the oral cavity, offering improved patient compliance and faster onset of action compared to conventional oral solid dosage forms. The present study was undertaken to design, develop, and evaluate fast-dissolving tablets of Glipizide, a second-generation sulfonylurea used in the management of Type-2 Diabetes Mellitus. Glipizide fast-dissolving tablets were formulated by the direct compression method using different superdisintegrants, namely crospovidone, croscarmellose sodium, and sodium starch glycolate, at varying concentrations. Preformulation studies were conducted to assess the physicochemical properties of the drug, and drug–excipient compatibility was evaluated using FTIR spectroscopy. The prepared formulations were evaluated for pre-compression parameters, post-compression characteristics, wetting time, disintegration time, drug content, and in-vitro dissolution behavior. Among the ten formulations developed, formulation F10 containing a combination of crospovidone and croscarmellose sodium exhibited the shortest disintegration time, rapid wetting, and nearly complete drug release within a short duration. Accelerated stability studies carried out as per ICH guidelines confirmed the physical and chemical stability of the optimized formulation. The study concludes that Glipizide fast-dissolving tablets prepared by direct compression represent a promising, patient-friendly alternative to conventional tablets, with potential benefits in terms of rapid onset of action and improved therapeutic compliance.
Sustained release tablets of antihypertensive drugs: A review
Hypertension is a chronic cardiovascular disorder that requires long-term and consistent pharmacotherapy to prevent serious complications such as stroke, myocardial infarction, heart failure, and renal damage. Conventional immediate-release antihypertensive dosage forms often require multiple daily administrations, resulting in fluctuating plasma drug concentrations, increased incidence of dose-related adverse effects, and poor patient compliance. Sustained release (SR) tablets have emerged as an effective strategy to overcome these limitations by providing controlled and prolonged drug delivery over an extended period. Sustained release tablets are designed to maintain therapeutic plasma drug levels, minimize peak–trough fluctuations, and reduce dosing frequency, thereby improving patient adherence and overall therapeutic efficacy. Antihypertensive drugs are particularly suitable for sustained release systems due to the chronic nature of hypertension and the need for continuous blood pressure control. Several classes of antihypertensive agents, including beta-blockers, calcium channel blockers, angiotensin-converting enzyme inhibitors, angiotensin receptor blockers, and centrally acting agents, have been successfully formulated into sustained release dosage forms. This review provides a comprehensive overview of sustained release tablets of antihypertensive drugs, highlighting the rationale for sustained drug delivery, ideal drug candidates, formulation approaches, polymers used, mechanisms of drug release, evaluation parameters, and kinetic modeling. The advantages, limitations, recent advances, and future prospects of sustained release antihypertensive formulations are also discussed. Sustained release tablet technology represents a significant advancement in the management of hypertension by improving patient compliance, enhancing therapeutic outcomes, and reducing cardiovascular risk.
Fast disintegrating tablets: An updated review on formulation and evaluation
Fast Disintegrating Tablets (FDTs), also referred to as Orally Disintegrating Tablets (ODTs) or Mouth-Dissolving Tablets (MDTs), are solid dosage forms designed to disintegrate rapidly in the oral cavity without the need for water. These tablets offer significant advantages in patient compliance, especially for pediatric, geriatric, and dysphagic populations, and provide faster onset of action compared to conventional tablets. This review presents an updated overview of the formulation strategies, technological approaches, evaluation parameters, and recent advancements in FDT development. Different formulation techniques—including direct compression, freeze-drying, sublimation, spray drying, molding, mass extrusion, and patented processes—have enabled the production of robust, fast-acting tablets with superior organoleptic properties. The selection and mechanism of superdisintegrants, such as Crospovidone, Croscarmellose Sodium, Sodium Starch Glycolate, Kyron T-314, and β-Cyclodextrin, play a critical role in achieving rapid disintegration and optimal mechanical strength. Taste-masking approaches, encompassing polymer coating, drug–resin complexes, microencapsulation, and cyclodextrin inclusion complexes, further enhance patient acceptability. Key evaluation parameters—including hardness, friability, drug content, wetting time, disintegration time, and dissolution profile—are essential to assess product quality and performance. Recent innovations such as 3D-printed FDTs, nanoparticle-loaded systems, and QbD-driven optimization have advanced the field significantly. This review consolidates current knowledge and provides insights into emerging trends, highlighting the potential of FDTs as a versatile and patient-friendly dosage form in modern pharmaceutical therapy.
Formulation and Evaluation of Fast Dissolving Tablets of Meloxicam Using Superdisintegrants
Fast Dissolving Tablets (FDTs) have gained significant attention due to their convenience, rapid onset of action, and suitability for dysphagic patients. Meloxicam, a BCS Class II drug, suffers from poor aqueous solubility and delayed onset when administered through conventional tablets. The present study aims to formulate and optimize Meloxicam FDTs using various superdisintegrants, including Sodium CMC, Crospovidone, Kyron T-314, and β-Cyclodextrin, with menthol sublimation employed to enhance porosity. Tablets were prepared using the direct compression method and evaluated for pre-compression parameters, post-compression characteristics, disintegration time, and in-vitro drug release. Among all formulations, batch F9 (containing Crospovidone + β-Cyclodextrin) exhibited the fastest disintegration time (≈9 seconds) and highest cumulative drug release (≈99.88% within 10 minutes). The optimized formulation outperformed the marketed tablet across all evaluation parameters. Thus, Meloxicam FDTs prepared with Crospovidone and β-Cyclodextrin provide a reliable, fast-acting, and patient-friendly alternative to conventional dosage forms.
Formulation and evaluation of a mucoadhesive buccal drug delivery system of Atomoxetine hydrochloride for improved bioavailability
Atomoxetine Hydrochloride (ATX HCl), a selective norepinephrine reuptake inhibitor (SNRI), suffers from low oral bioavailability due to extensive hepatic first-pass metabolism and bitter taste, limiting compliance in pediatric ADHD patients. The present study aimed to formulate and evaluate a mucoadhesive buccal drug delivery system of ATX HCl to overcome these limitations. Preformulation studies established physicochemical compatibility between the drug and selected polymers (HPMC K15M, Carbopol 934P, PVP K30). A drug–resin complex (DRC) utilizing Tulsion 339 (1:2 ratio) was prepared for taste masking. Buccal films were fabricated using the solvent casting method and optimized through systematic variation of polymer and plasticizer ratios. The optimized formulation (F3) exhibited excellent mechanical properties, neutral surface pH, satisfactory mucoadhesive strength (17.8 g), and sustained drug release (91% in 6 h), following Higuchi kinetics (R² = 0.994) with non-Fickian diffusion (n = 0.62). Ex vivo permeation across porcine buccal mucosa confirmed 82% permeation within 6 h. Analytical methods (UV at 272 nm and HPLC at t_r = 3.9 minutes) were validated as per ICH Q2(R2). Accelerated stability studies revealed no significant changes in drug content, appearance, or release profile over 6 months. The findings demonstrate that the developed mucoadhesive buccal film offers a promising alternative to conventional oral therapy by enhancing bioavailability, controlling release, masking bitterness, and improving patient compliance.
Development and characterization of Luliconazole ethogel for topical use in the treatment of athlete’s foot infection
Luliconazole is an imidazole antifungal agent with a unique structure, as the imidazole moiety is incorporated into the ketene dithioacetate structure. To develop and optimize the ethosomal formulation of luliconazole for Athlete’s foot infection. Characterization of optimized formulation in vitro. To develop and characterize luliconazole ethosomes loaded topical gel (Ethogel). Anti–fungal study of the optimized ethogel formulation. That ethosomes can become a promising drug carrier in future for not the only topical treatment of local and systemic disorders, but also for the cosmetic and cosmeceutical fields. The present study focused on the development and characterization of LCZ-loaded ethogel and they’re in incorporation in the topical gel to increase the permeation through stratum corneum, imparting controlled release as well as enhancing the hydration of the skin. Therefore, LCZ loaded ethosomes were prepared by Cold method with high-speed homogenization combined with ultra-sonication. The particle size was found to be in the range of 185 to 289 nm and a maximum of 93 % EE and -24.49 mV Zeta potential. ATR and XRD data ruled out any possible incompatibility among the excipient. Release studies confirmed the sustained release nature of ethosomes.
Formulation & evaluation of Voriconazole nanoparticles for ophthalmic drug delivery system
Voriconazole is a second-generation antifungal agent with excellent broad spectrum of antifungal activity commercially available for oral and intravenous administration. Systemic administration of voriconazole is associated with side effects including visual and hepatic abnormalities. This study assessed the feasibility of using solid lipid nanoparticles for ocular delivery of voriconazole adopting stearic acid as lipidic material, tween 80 as a stabilizer, and Carbopol 934 as controlled release agent and for increasing the precorneal residence time in eye. The systems were prepared using two different methods, that is, ultrasonication method and microemulsion technique. The results indicated that the larger particle size of SLNs was foundwith microemulsion technique (308±3.52nm to 343±3.51) compared to SLN prepared with ultrasonication method (234±3.52nm to 288±4.58 nm). The polydispersity index values were less than 0.3 for all formulations and zeta potential of the prepared formulations by these two methods varied from −22.71 ± 0.63 mV to −28.86 ± 0.58mV. Powder X-ray diffraction and differential scanning calorimetry indicated decrease in crystallinity of drug. The in vitro release study and the SLN formulations prepared with ultrasonication method demonstrated sustained release up to 12 hours. This study demonstrated that SLN prepared by ultrasonication method is more suitable thanmicro emulsion technique without causing any significant effect on corneal hydration level.
Formulation and charecterization of blend microsphere of Glipizide
The purpose of this research was to formulate and system atically evaluate in vitro and in vivo performances of mucoadhesive microspheres of glipizide. Glipizide micro spheres containing chitosan were prepared by simple emulsification phase separation technique using glutaraldehyde as a cross-linking agent. Results of preliminary trials indicate that volume of cross-linking agent, time for cross-link ing, polymer- to-drug ratio, and speed of rotation affected characteristics of microspheres. Microspheres were discrete, spherical, and free flowing. The microspheres exhib ited good mucoadhesive property in the in vitro wash-off test and also showed a high percentage drug entrapment efficiency. A 32 full factorial design was employed to study the effect of independent variables, polymer-to-drug ratio (X1), and stirring speed (X2) on dependent variables percentage mucoadhesion, t80, drug entrapment efficiency, and swelling index. The best batch exhibited a high drug entrapment efficiency of 75% and a swelling index of 1.42; percentage mucoadhesion after 1 hour was 78%. The drug release was also sustained for more than 12 hours. The pol ymer-to-drug ratio had a more significant effect on the dependent variables. In vivo testing of the mucoadhesive microspheres to albino Wistar rats demonstrated significant hypoglycemic effect of glipizide.
Optimization and evaluation of Venlafaxine hydrochloride fast dissolving oral films
Three factors, three level full factorial design was used to develop venlafaxine HCl fast dissolving oral films (FDOFs) to optimize the concentrations of the film forming polymer; hydroxypropyl methylcellulose HPMC (X1), super disintegrant; sodium starch glycolate SSG, (X2) and glycerol as the film plasticizer (X3). Effects of the three factors on the disintegration time (Y1), swelling index (Y2), and dissolution efficiency at 15 min; DE%15 (Y3) of the prepared FDOFs were evaluated by using statistical models. The optimized film formula was characterized in term of x-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and morphological characteristics. Disintegration time was found to increase with the increase in HPMC (X1) concentration, and the shortest disintegration time (21.67 ± 2.08 s) was observed in case of F2 formula (lowest HPMC level and highest glycerol level in absence of SSG). The highest swelling index (3.64 ± 0.59) was observed in case of film formula F1 (medium concentrations of both HPMC and glycerol and highest SSG concentration. The results also indicated that as the concentration of HPMC increased the DE%15 decreased. SSG (X2), with highest value (72.33 ± 1.71%) was recorded for in case of F12 (using 2% HPMC, 5%SSG and 1.5% glycerol). The optimized FDOF formula derived by the statistical models suggested 2% HPMC, 5% SSG, and 1% glycerol. The data obtained from DSC and XRPD revealed no interaction between drug and FDOT excipients. In addition, XRPD studies proved that the venlafaxine HCl was homogeneously dispersed in the film matrix.
Formulation And Characterization of Colon Targeting Drug Delivery of Etoricoxib
Objective: Design and development of okra gum-based colon specific tablet formulations for chrono therapeutic delivery of drugs, Eterocoxib for the treatment of diseases. Materials and methods: The gum extracted from thoroughly washed, sliced and crushed fruits with a laboratory blender. After extraction the precipitate of the gum were dried in hot air oven for about 20min at 50C and then precipitates were kept in a dessicator for further drying Etoricoxib, HPMC, E.C other formulation excipients. The in vitro dissolution test has been performed in 0.1 N HCl for first two hours and the rest in 6.8 pH phosphate buffer using USP apparatus type II (paddle), at 50 rpm for six hours. The spectrum was measured in the solid state as Potassium bromide dispersion. The Press coated tablets were prepared by varying polymer (HPMC): polymer (E.C) ratio i.e., 4:0, 3:1, 2:2, 1:3, 3:1 and 0:4. Results and conclusion: The drug release from the dosage forms was started after 4hrs lag time. The Press coated tablets obtained by 3:1 ratio(P2F9) shows good lag time, more % drug released immediately after lag time in comparision with those prepared by4:0, 2:2, 3:1, 0:4 hence P2F9. It has been concluded from the above investigation that Press coated dosage form of Etoricoxib could delay the release up to 4hrs and further exhibited immediate release of the drug and shows 20 hr action. The results obtained in this research work clearly indicated a promising potential of colon specific drug delivery of eterocoxib by using okra gum containing HPMC, HPMS EC, as a rate controlling polymer for the effective treatment of rheumatoid patients.
Formulation and Characterization of Zingiberol Loaded Microsphere for Motion Sickness
The present research work involve the development of Zingiberol as the treatment of motion sickness. The Zingiberol microsphere was formulated by Ionotropic gelation method using different polymers in different ratio depending on RSM method. The prepared formulations were optimized on the basis of dependent variables like particle size (mg), entrapment efficiency etc. The SEM photographs of Zingiberol microsphere before dissolution shows the spherical and smooth surface whereas after dissolution the pores and crevices were shown which is indicating that the microsphere are showing drug release by diffusion mechanism. The microsphere formulations were able to sustain the release of drug both in vitro and in vivo. In the stability studies no significant change in drug entrapment release characteristics of the microspheres.
Copyright (c) 2019 International Journal of Advances in Pharmaceutics
A Review on Niosomes - A novel approach for drug targeting
This is a general review on niosome as drug carrier, which improves the bioavailability of drugs, increases penetration through skin, releases drug in a controlled or sustained manner, and used for targeting of drugs to specic sites in the body.Niosomal drug delivery system can be considered as an emerging novel drug delivery system, which consists of microscopic non-ionic vesicles composed of non-ionic surfactants. These are biodegradable, relatively nontoxic, more stable and inexpensive, and an alternative to liposomes. Methods of preparation, characterisation and application of niosomes have been reviewed. Niosome has potential to reduce the side effects of drugs and increase therapeutic effectiveness in various diseases. It can also be used as a carrier to deliver drugs topically. This review presents an overview of the types of niosomes, techniques of preparation of niosome characterisation and their applications.
Simultaneous estimation of aspirin and omeprazole in laboratory sample by different UV spectrophotometric techniques
The aim of the present work is to develop simple, precise and economic UV- spectrophotometric methods for the simultaneous estimation of aspirin and omeprazole laboratory sample. The absorbance maxima (?max) for detection of aspirin and omeprazole were selected as 274 nm and 302 nm respectively for simultaneous equation method while wavelength range for detection of aspirin and omeprazole were selected as 270 nm - 276 nm and 300 nm - 305 nm respectively for area under curve method. Absorbance ratio method uses the ratio of absorbances at two selected wavelengths, one which is an isoabsorptive point and other being the ? max of one of the two components. From the overlay spectra of two drugs, it is evident that aspirin and omeprazole show an isoabsorptive point at 238.6 nm. Zero crossing first derivative spectrophotometry, where Aspirin showed zero crossing point at 301nm and Omeprazole showed zero crossing point at 274nm. Linearity for Aspirin was between 25- 125 ?g/mL and Omeprazole was 3-15 ?g/mL. These methods were successfully applied for estimation of Aspirin and Omeprazole in laboratory sample.
First derivative zero crossing point method
Formulation, development, and evaluation of Silymarin loaded topical gel for fungal infection
The objective of work was the formulation of Silymarin Loaded Topical gel obtained from the seeds of plant Silybum Marianum (L). Silymarin is a composition of flavolignan. It includes Silibinin, Silydianin, Silychristin, and isosilybinin. silymarin is used as Hepatoprotective, Antioxidant, Anticancer, Anti-Inflammatory, Anti-fibrotic, Immunomodulatory a Liver Regenerating action. It also used in viral hepatitis neuroprotective and Neurotropic action. The different type of formulation available in tablet, capsule, syrup, suspension, nanoparticles in the market. The aim of the study was to formulate and develop silymarin Loaded gel and to check its Antipsoriasis activity, with the use of Methanol as co-solvent the HPMC as Gel forming Agent and Methyl paraben and propyl paraben as Preservative. The glycerin acts as Humectant and Tween 80 used as a surfactant. The Characterization of gel such as pH, Drug content, spreadability, viscosity, in-vitro drug release was carried out in pH 6, Primary skin irritation test and antifungal activity were checked. The drug content was found to be 95.8%. Spreadability of the gel was found to be 20.66gm cm/sec. The pH of silymarin loaded gel was found to be 6.9. The silymarin loaded gel shows the pseudoplastic flow from the rheogram. It shows Drug release 96.08% over a period of 3h. There was no acute skin irritancy found.
Inclusion of Hydrophilic-Lipophilic Balance (HLB) in the treatment of Psoriasis- A new approach
The present study highlights the importance of Hydrophillic-Lipophilic value of the base cream for the dermatological purposes beyond formulation stability. Hydrophilic- Lipophilic Balance (HLB) is largely considered for attaining stability of the base cream by the chosen emulsifier/ surfactants. However the base formulation (cream or ointment) also must act as an emulsifier to balance the hydrophilic- lipophilic ecosystem of the skin besides the formulation acts as the drug dispensing mechanism. Psorolin ointment for the treatment of psoriasis is being formulated with due diligence to HLB value due to the skin conditions of psoriasis. Details are presented in the paper.
A review on recent advancement in liquisolid techology
Liquisolid technique is a novel process in which a liquid can be converted into a material that flows freely, is readily compressible. The carrier material in liquisolid compact comprises the liquid part, which is the liquid drug or a drug solution in liquid vehicles that are non-volatile. Solubility is the main parameter in the circulation of blood to achieve the whole concentration of the drug for pharmacological action. The rate of dissolution of drugs enhances in liquisolid technology. This in turn increases absorption and bioavailability subsequently. This review discusses the different advances and changes to improve liquisolid technology formulations and enhancement of dissolution rate of poorly soluble drugs. Most of the new chemical entities have high lipophilicity and poor water solubility, resulting in poor bioavailability. The release rate of these drugs should be increased in order to improve bioavailability. The technique is based on dissolving the insoluble drug in the solution loaded with non-volatile solvent. Then the dissolution rate of drug which is poorly soluble will rise. The enhanced bioavailability is due to the increased surface area of drug for release, increased drug aqueous solubility or improved wetting capacity.