Journal of Drug Discovery and Therapeutics

Formulation, Development of Organogel Containing Dexamethasone and Diclofenac for the Treatment of Inflammation

2026-05-01T04:21:21+00:00

The present study aimed to develop and evaluate an organogel formulation containing dexamethasone and diclofenac for topical drug delivery to enhance anti-inflammatory activity and improve patient compliance. Organogels were prepared using different polymers such as Carbopol 934, HPMC, and Tween 80 in varying concentrations. A total of nine formulations (F1–F9) were developed and evaluated for physicochemical parameters including pH, viscosity, spreadability, gel strength, drug content uniformity, and in vitro drug release. Pre-formulation studies confirmed the purity and compatibility of drugs using FTIR, UV spectroscopy, and melting point determination. The pH of all formulations was found within the acceptable range (6.1–6.7), indicating suitability for topical application. Viscosity and spreadability results showed that formulations exhibited good consistency and ease of application. Drug content uniformity ranged from 97.5% to 101%, confirming uniform distribution.

In vitro drug release studies revealed that formulation F7 showed the highest drug release (98.7% at 8 hours). Drug release kinetics followed the Higuchi model, indicating diffusion-controlled release. Thus, the developed organogel formulation can be considered a promising topical drug delivery system for effective management of inflammation.

Keywords: Organogel, Dexamethasone, Diclofenac, Topical drug delivery, Drug release kinetics.

Formulation and Evaluation of Sustained Release Pellets of Antihypertensive Drug

2026-05-10T16:05:56+00:00

Objective: The aim of the present study was to formulate sustained-release pellets of bosentan by eudragit RL 100 and RS 100, which are the polymers used in the pan coating technique.

Methods: The sustained release pellets of bosentan were formulated by pan coating method. The drug was coated on nonpareil seeds along with EudragitRL100 by solution layering technique. Drug-loaded pellets were coated with EudragitRS100. The prepared pellets were evaluated for moisture content, drug content, particle size, and in vitro drugrelease. Stability studies were carried out on the optimised formulations for a period of 6 mo.

Results: The drug content was in the range of 98.89±0.32. The mean particle size of the drug-loaded pellets was in the range of 835 μm. The drug release rate decreased as the concentration of eudragit increased in the pellet formulations.Among the prepared formulations, PC 4 showed

89.35±0.52 drug release in 12 h from a good linear relationship was established between model-independent approaches (T25%, T50%, and T100%) and weight gain in coating. This indicated the possibility of extending the drug release by increasing the weight gain in the coating, and hence, it was proposed to extend the drug release for 24 h. From the prepared pellets, the optimised formulation PC 12 showed a 100.02±0.03 drug release in 24 h. Furthermore, these pellets were filled into capsules and compared the dissolution studies. The compatibility between drugs and polymers in the drug-loaded pellets was confirmed by DSC and FTIR studies. Stability studies indicated that the pellets were stable.

Conclusion: The prepared pellets were capable of releasing the drug for 24 h to treat the Pulmonary ArterialHypertension.

Keywords: Pellets, Pan coating, Eudragit, Bosentan, Independent model.

Cubosomes in Transdermal Drug Delivery System

2026-05-13T04:24:56+00:00

Cubosomes are spherical, cubic particles characterized by an internal cubic lattice. Cubosomes possess an extensive interfacial area and feature two internal aqueous channels divided by honeycombed features. They exhibit thermodynamic stability. The cubic liquid crystalline particles are known as cubosomes. These particles consist of particular surfactants, which have a unique microstructure, making them useful and possessing an ideal water content ratio. The cubic liquid crystalline phase is transparent, highly viscous, and features a distinctive nanoscopic structure. "Bicontinuous" indicates a lipid bilayer assembled in a space-filling system separating two continuously existing but not overlapping aqueous regions. Cubosomes are usually created through hydration of either a polar lipid or a surfactant, generating the cubic phase and dispersing the solid-like phase into tiny particles. From the time of their discovery and naming, cubosomes self-assembled have attracted considerable attention as potent drug delivery systems. They have distinct drug-loading mechanisms and different cubic shapes and composition inside. Their properties include high internal surface area, cubic crystalline structures, lipids' biodegradability, encapsulation of hydrophobic, hydrophilic, and amphiphilic compounds, targeted delivery, and bioactive substance release. Cubosomes can be classified using several evaluation parameters and have broad applications in diverse fields. Cubosomes are consequently garnering heightened interest within the pharmaceutical sector.

Keywords: amphiphilic, hydrophilic, hydrophobic, drug-loading,

Hydrotropy: A Promising Solubilization Technique for Poorly Water-Soluble Drugs

2026-05-13T04:32:22+00:00

The low aqueous solubility has continued to be one of the greatest challenges in the current pharmaceutical sciences since a great percentage of the emerging therapeutic molecules are characterized by low water solubility and dissolution-limited absorption. Drugs that fall under Biopharmaceutics Classification System (BCS) Class II and IV are often characterized by poor dissolution properties, unpredictable oral bioavailability, slow absorption and unpredictable therapeutic effects. Traditional methods of solubility enhancement like micronization, salt formation, co-solvency, surfactant system, cyclodextrin complexation, solid dispersions and nanotechnology-based methods have demonstrated a lot of success but are also accompanied by some limitations like toxicity, solvent contamination, high cost of production, physical instability and complicated scale-up processes. Hydrotropy has become a cost-effective, environmentally friendly, and industrially viable alternative to enhance aqueous solubility of poorly water-soluble drugs. Hydrotropic agents, including sodium benzoate, sodium salicylate, sodium citrate, nicotinamide, and urea, enhance solubility and increase the wettability via self-aggregation, hydrogen bonding, π–π interactions, solvent structure alteration, and solubility enhancement. Recent developments in mixed hydrotropy also enhanced pharmaceutical applications by decreasing toxicity, and augmenting synergistic solubilization effects. Hydrotropic systems have proved to be widely applicable in oral, parenteral, topical, transdermal, ocular and analytical preparations. This review critically discusses the historical background, mechanisms, classifications, pharmaceutical applications, advantages, limitations, comparative evaluation, and future perspectives of hydrotropic solubilization. Mixed hydrotropy and green pharmaceutical manufacturing have been given a special focus.

Keywords: Hydrotropy, mixed hydrotropy, poorly water-soluble drugs, solubilization enhancement, bioavailability, hydrotropic agents, pharmaceutical formulation

Formulation, Development and Evaluation of Antifungal Shampoo of Itraconazole with Natural Extract

2026-05-01T04:25:55+00:00

The present study aimed to formulate and evaluate an antifungal shampoo containing itraconazole in combination with natural extracts such as neem, aloe vera, reetha, and shikakai for effective treatment of scalp fungal infections. A total of nine formulations (F1–F9) were developed using aqueous gel-based emulsion technique by varying concentrations of herbal components. Preformulation studies including DSC and FTIR confirmed the purity and compatibility of itraconazole with excipients. The prepared shampoos were evaluated for physicochemical parameters such as pH, viscosity, spreadability, foamability, stability, and drug content. The pH of all formulations ranged from 5.4 to 6.1, suitable for scalp application. Viscosity varied depending on xanthan gum concentration, with F3, F6, and F9 showing higher viscosity. Spreadability and foaming studies indicated good cleansing and application properties. Among all formulations, F6 exhibited optimal performance with balanced viscosity, stable foam, and good spreadability. In vitro drug release studies revealed sustained release of itraconazole up to 79% over 8 hours. Drug release kinetics followed first-order model (R² = 0.998), indicating concentration-dependent release. The formulation also showed significant antifungal activity against fungal strains. Thus, the developed antifungal shampoo represents a promising topical delivery system combining synthetic and herbal agents.

Keywords: Itraconazole, Antifungal shampoo, Herbal extract, Neem, Aloe vera, Drug release kinetics.

Analytical Method Development and Validation of Glimepiride in Tablet Dosage Form by New RP-HPLC

2026-05-08T06:58:23+00:00

A simple, precise, accurate, and stability-indicating reverse-phase high-performance liquid chromatographic (RP-HPLC) method was developed and validated for the quantitative estimation of Glimepiride in tablet dosage form. Chromatographic separation was achieved using a C18 column (250 mm × 4.6 mm, 5 µm) with an isocratic mobile phase consisting of Acetonitrile: Phosphate Buffer (pH 3.0) in the ratio of 60:40 (v/v) at a flow rate of 1.0 mL/min. Detection was carried out at 230 nm using a UV/PDA detector. Under optimized chromatographic conditions, Glimepiride showed a sharp and symmetrical peak with a retention time of approximately 5.8 minutes.

The developed method was validated according to ICH Q2(R1) guidelines for parameters such as system suitability, linearity, accuracy, precision, robustness, limit of detection (LOD), and limit of quantification (LOQ). The method exhibited excellent linearity in the concentration range of 10–60 µg/mL with a correlation coefficient (r² = 0.9994). The %RSD values obtained for intraday and interday precision studies were 0.48% and 0.62%, respectively, indicating good repeatability and reproducibility of the method. Accuracy studies performed by recovery method at 80%, 100%, and 120% levels showed mean recovery of 99.73%, confirming the reliability of the developed method. The calculated LOD and LOQ values were found to be 0.85 µg/mL and 2.58 µg/mL, respectively, demonstrating good sensitivity of the method. Robustness studies revealed that small deliberate changes in chromatographic conditions such as flow rate and wavelength did not significantly affect analytical performance.

The developed RP-HPLC method was found to be simple, rapid, precise, accurate, economical, and suitable for routine quantitative analysis of Glimepiride in bulk drug and marketed tablet dosage forms. The method can also be effectively applied for quality control analysis and stability studies in pharmaceutical industries.

Keywords: Glimepiride, RP-HPLC, Method validation, Stability-indicating method, Tablet dosage form, ICH guidelines

Formulation and In Vitro Evaluation of Propranolol Hydrochloride Sublingual Films for Effective Hypertension Control

2026-05-10T12:04:29+00:00

The objective of the present investigation was the formulation and evaluation of an oral fast-dissolving sublingual film of Propranolol HCl. This study aimed to formulate a rapid dissolving sublingual film of propranolol HCl by employing HPMC E15 as a film-forming agent, propylene glycol as a plasticizer, and cross-povidone as a disintegration agent. A fast-dissolving film was fabricated using the solvent casting technique. The stability studies of the patch were conducted for the optimized batch in accordance with the ICH guidelines. The medication and excipients underwent characterization according to the Indian Pharmacopoeia (IP). Investigation of drugs and excipients using Fourier Transform Infrared Spectroscopy (FT-IR). The films underwent physicochemical characterization, including assessment of weight Variation, thickness, tack test, drug content homogeneity, surface pH, folding endurance, disintegration time, in vitro drug release, and stability testing. Out of all the formulas (F1 to F9) that were created, batches F4 and F5 exhibited the highest quality, with a release of 109.86% and 104.73%, respectively during a 10-minute timeframe. The statistically optimized formulation was assessed using FT-IR (Fourier transform-infrared spectroscopy) investigations, which revealed no chemical interactions between the medication and polymer. Therefore, the propranolol HCl quick-dissolving film may serve as a superior substitute for tablets and capsules in achieving better oral bioavailability for the management of hypertension.

Keywords: Fast dissolving sublingual film, Propranolol HCl, solvent casting method, Drug release, Fast onset of action.

Pharmaceutical Development and Analytical Method Validation of a Nicotine Polacrilex-Containing Pouch Formulation

2026-05-10T13:02:09+00:00

Nicotine Polacrilex is a most commonly used active pharmaceutical ingredient in the treatment of tobacco dependence as a nicotine replacement therapy (NRT) in adult patients. This paper demonstrates the pharmaceutical development and analytical method validation of a novel nicotine polacrilex-containing pouch formulation through buccal nicotine delivery. This formulation was designed to deliver 2 mg of nicotine per pouch through controlled buccal absorption, providing a smokeless, tar-free alternative to cigarettes.

Keywords: Nicotine polacrilex, nicotine replacement therapy, pouch formulation, buccal drug delivery, HPLC method validation, ICH Q2, smoking cessation, tobacco dependence.

Formulation and Evaluation of Extended-Release Glipizide Capsules Using Ethyl Cellulose and HPMC K100M for Once-Daily Oral Delivery

2026-05-12T05:18:19+00:00

Glipizide is a second-generation sulfonylurea used in the management of type 2 diabetes mellitus, but its short elimination half-life and poor aqueous solubility make it a suitable candidate for extended-release oral drug delivery. Hydrophilic-hydrophobic matrix systems based on hydroxypropyl methylcellulose (HPMC) and ethyl cellulose (EC) are widely used to modulate drug release through combined diffusion, swelling, and matrix relaxation mechanisms.

Objective: The study aimed to develop and evaluate extended-release matrix capsules of glipizide using different EC:HPMC K100M ratios and to identify an optimized formulation capable of sustained release over 24 hours.

Formulation and Evaluation of Gastro-Retentive Effervescent Floating Tablets of Ranitidine Hydrochloride Using HPMC K100M as a Rate-Controlling Polymer

2026-05-12T05:23:48+00:00

Background: Ranitidine hydrochloride (HCl), a Histamine H₂-receptor antagonist, exhibits pharmacokinetic limitations including a short biological half-life (2–3 h), narrow absorption window confined to the upper gastrointestinal tract, and low oral bioavailability (~50%), necessitating twice- daily conventional dosing. A gastro-retentive floating drug delivery system (GFDDS) offers a rational approach to prolong gastric residence, sustain drug release, and improve bioavailability.

Objective: To develop and evaluate effervescent floating matrix tablets of Ranitidine HCl using HPMC K100M as a hydrophilic rate-controlling polymer and sodium bicarbonate as a gas-generating agent, with the goal of achieving once-daily therapeutic delivery.

Methods: Six formulation batches (F1–F6) were prepared by direct compression with systematically varied HPMC K100M (30–50% w/w) and NaHCO₃ (10–17.5% w/w) concentrations at a fixed Ranitidine HCl dose of 150 mg. Tabletswere evaluated for preformulation characterisation (FTIR, DSC, UV spectrophotometry), pre-compression flow properties, post-compression pharmacopoeial parameters, in vitro buoyancy, in vitro drug release (USP Type II, 0.1N HCl, 24 h), drug release kinetic modelling, and accelerated stability (40°C/75% RH, 3 months, ICH Q1A(R2)).

Results: FTIR and DSC confirmed absence of drug–excipient interactions. Batch F3 (HPMC K100M 40%, NaHCO₃15%) was identified as the optimised formulation with floating lag time (FLT) of 1.9 ±

0.2 min, total floating time (TFT) of 19.4 ± 0.7 h, drug release of 19.8% at 1 h and 96.8% at 24 h, and anomalous (non-Fickian) drug transport (Korsmeyer–Peppas n = 0.543, R² = 0.9968). Stability testing confirmed drug content ≥ 97.9% with unchanged release profiles (f₂ > 50) over 3 months.

Conclusion: A once-daily effervescent floating tablet of Ranitidine HCl was successfully developed using directly compressible excipients. Batch F3 fulfilled all buoyancy, release, and stability criteria, demonstrating the feasibility of GFDDS for bioavailability enhancement of narrow-absorption-window drugs.

Keywords: Gastro-retentive drug delivery; floating tablets; Ranitidine hydrochloride; HPMC K100M; sodium bicarbonate; effervescent; controlled release; floating lag time.