PVP K30 Research Articles

Improve the solubility of cefpodoxime proxetil by amorphous solid dispersion technique

This research aimed to improve the solubility and stabilize cefpodoxime proxetil (CP), a class IV drug, by amorphous solid dispersion (ASD) technique. Four formulations were prepared by dispersing amorphous CP in soluplus, polyvinylpyrrolidone (PVP K30), and ethyl cellulose (EC) blends in different compositions and ratios. The optimum formulation was stored in accelerated conditions at 40 °C and 75% relative humidity for six months. The drug's solubility and dissolution rate in different systems were explored. Furthermore, Differential Scanning Calorimetry (DSC), X-ray Powder Diffractometry (PXRD), Fourier Transform Infrared spectroscopy (FTIR), and Field Emission Scanning Electron Microscopy (FESEM) were used to examine the physical state of the drug. The antibacterial activity of the drug was evaluated during the experiment. When mixing CP with soluplus and PVP K30 in a 1:1:1 ratio as ASD, the drug solubility at pH 1.2 enhanced about 28 folds than a pure drug, and the dissolution rate increment was observed. The DSC, FTIR, and PXRD data confirmed the drug is amorphous and miscible with these polymers. FESEM revealed particle size reduction. The antibacterial activity was raised. After storage in the accelerated condition, physical investigations indicated that no recrystallization occurred, and this condition had little effect on in vitro drug dissolution and antibacterial activity. This can be a good indicator of the drug's solubility enhancement and physical stability optimization that will make the possibility of preparing this drug in the future as an oral solid dosage form with the possibility of manufacturing with a drug company due to the promising results.

Development and Evaluation of Huperzine A-Loaded Microneedles for Transdermal Delivery and Pretreatment of GD Poisoning.

Huperzine A (Hup A), a reversible acetylcholinesterase inhibitor, shows protective potential against neurotoxic poisoning. Current formulations (oral tablets/capsules and injectables) face limitations: oral administration suffers from first-pass metabolism and fluctuating plasma concentrations due to frequent dosing, while injectables require sterile administration, reducing long-term compliance. The aim of this study was to prepare dissolving microneedles (MNs) patches containing Hup A for pretreatment against soman (GD) poisoning. Hyaluronic acid (HA), polyvinylpyrrolidone K30 (PVP K30) and sorbitol were selected as matrix materials in specific proportions and concentration ranges based on single-factor screening experiments and orthogonal design optimization. In order to further evaluate the potential of the Hup A MNs, optimized formulations were selected for subjected to characterization. This evaluation encompassed morphological observation, mechanical properties, skin penetration efficacy, recovery time, in vitro drug release study, permeability assays, pharmacokinetic study, and pharmacodynamic study. Statistical analyses were performed using Student's t-tests for pairwise comparisons and one-way ANOVA for multiple comparisons. The results demonstrated that prepared Hup A MNs had a conical shape with a smooth surface and sharp tips. Hup A MNs had sufficient mechanical strength (122.3 ± 15.3 N) to penetrate through the skin and could be quickly skin of recovery 6min. In permeability assays, the cumulative Hup A release was about 35.4μg at 2h and 58μg at 10h. Pharmacodynamic results demonstrated that compared to oral administration, Hup A MNs reduced the onset time (30min vs. 60min) and extended the effective prevention duration against GD poisoning (6h vs. 2h). Pharmacokinetic analysis showed that MNS administration can maintain a more lasting and stable blood concentration as compared to oral administration. MNs are a valuable drug delivery system, benefiting the patients with minimal skin invasion. Taken together, these results demonstrated that Hup A-loaded MNs are acquiring a new alternative for pretreatment of OPNAs.

Evaluating polymer influence on resuspendability of indomethacin suspensions produced by microfluidization.

Evaluating polymer influence on resuspendability of indomethacin suspensions produced by microfluidization.

Minimally invasive treatment of fungal keratitis with voriconazole microneedle corneal patch.

Minimally invasive treatment of fungal keratitis with voriconazole microneedle corneal patch.

Enhancing gliclazide solubility using solid dispersions with carboxymethyl chitosan and polyvinylpyrrolidone K30 as polymeric carriers

Background Gliclazide (Glz) is a second-generation sulfonylurea antidiabetic drug, used to treat type II diabetes mellitus. Glz is a class II drug according to the biopharmaceutic classification system (BCS), indicating that it has high permeability and poor aqueous solubility. Objective This study aimed to improve the solubility of Glz via the solid dispersion method. Methods Solid dispersions of the drug were formulated using carboxymethyl chitosan (CMch) and polyvinyl pyrrolidone K30 (PVP K30) in varying drug to carrier ratios (1:1, 1:3, and 1:5 w/w) using kneading and solvent evaporation methods. The solubility of Glz solid dispersions was compared with the pure Glz and co-grounded mixtures of the drug. Results Both carriers exhibited a noticeable increment in solubility and dissolution rate compared to the drug alone. Glz: CMch (1:5 w/w ratio) formulation made by the kneading method exhibited an increased solubility by approximately nine folds (337.79 ± 4.22 µg/ml) as compared to Glz alone (38.74 ± 4.69 µg/ml). However, the greatest improvement in drug dissolution rate was observed in the dispersion made with 1:5 w/w drug to PVP K30 using the solvent evaporation method, and the percentage drug release reached 100% after 30 min. Solid dispersions characterization manifested the compatibility between the drug and carriers, with alteration in particle morphology, and reduction in drug crystallinity. Conclusion Overall, solid dispersion using CMch has shown to be an excellent approach for enhancing the solubility and dissolution of the class II drug Glz.

Preparation and evaluation of gastroretentive floating unfolding film of baclofen

Baclofen, a muscle relaxant used for severe pain management, has a narrow absorption window limiting its bioavailability. Enhancing its gastric residence time could potentially improve its absorption and effectiveness. Floating drug delivery systems are a promising approach to prolong drug retention in the stomach. This study aimed to develop a floating bilayer film for the sustained release of baclofen. The core of the film was formulated with baclofen, PVP K90, sodium alginate, and PEG 400 as a plasticizer, while the controlled release layer contained Eudragit RS100 or RLPO with different plasticizers (DBP and PEG 400). All formulations were evaluated for weight uniformity, drug content, thickness, folding ability, swelling, and in vitro drug release. The optimized formula had a 98% drug release within 12 hours, floated effectively for 24 hours, and followed zero-order kinetics.

Formulation, Development and Evaluation of Novel Gastroretentive Sustaine Release of Ciprofloxacin HCl Floating Matrix Tablet

Drugs that have limited absorption window in the gastrointestinal tract will have poor absorption. For these drugs, gastro-retentive drug delivery systems offer the advantage in prolonging the gastric emptying time. The aim of formulating floating tablets of ciprofloxacin was to prolong the gastric residence time after oral administration to accomplish the controlled release of drug. Ciprofloxacin, a broad-spectrum fluoroquinolone antibacterial agent and it is use in the treatment of bone and joint infections, diarrhoeal infection, lower respiratory tract infections, urinary tract infections and meningococcal prophylaxis. Floating tablets of ciprofloxacin were prepared by direct compression method using different grades (K-15 and K-4) of Hydroxyl Propyl Methyl Cellulose (HPMC) and PVP K30 using effervescent technique. Sodium bicarbonate was incorporated as a gas-generating agent. The effect of citric acid on drug release profile and floating assets was also examined. FTIR studies adapted that there was no incompatibility between the polymers and the drug. Tablet pre-formulation parameters were within the pharmacopoeias limit. Tablets were estimated by different parameters such as weight uniformity, content uniformity, thickness, hardness, in vitro release studies, resistance determination and kinetic analysis of dissolution data. Tablet showed ≤ 1min lag time, continuation of resistance for >12 h. The in-vitro drug release pattern of optimized ciprofloxacin floating tablets (F7) was fitted to different kinetic models which showed highest regression (r2 =0.983) for first order kinetics. Ciprofloxacin floating tablets exhibited increased gastric residence time, there by improved bioavailability and therapeutic effect of the drug.

Formulation and optimization of upadacitinib-loaded transdermal patches for rheumatoid arthritis with zero-order release kinetics

Background: To develop and optimize Upadacitinib-loaded transdermal patches for rheumatoid arthritis treatment with improved patient compliance and sustained drug delivery. Methodology: Upadacitinib transdermal patches were formulated using a 3² factorial design approach with PVP K30 and HPMC K4M as key polymeric components. The patches were characterized for physicochemical, mechanical, and ex vivo permeation properties. Results and Discussion: The optimized formulation (SF8) exhibited excellent physicochemical characteristics, including high drug content (99.05 ± 0.83%), optimal mechanical properties with tensile strength of 0.912 kg/mm² and adhesion strength of 3.94 N. The ex vivo permeation reached 86.35% at 12h, with the flux of 102.91 μg/cm²/h following zero-order kinetics (R² = 0.9777). The experimental values closely matched predicted values with less than 2% error. Accelerated stability studies confirmed minimal changes in critical parameters over six months. Conclusion: The optimized Upadacitinib transdermal patch provides sustained drug delivery with zero-order release kinetics and excellent stability. This transdermal delivery system offers a promising alternative to oral therapy with potential advantages of improved patient compliance, reduced dosing frequency, and avoidance of first-pass metabolism for rheumatoid arthritis management

Exploring the Relationship Between Stability and Dynamics in Polymer-Based Amorphous Solid Dispersions for Pharmaceutical Applications.

Mixing polymeric excipients with drugs in amorphous solid dispersions (ASD) is known to enhance the bioavailability of drugs by inhibiting their recrystallisation. However, the mechanisms underlying stabilisation remain not fully understood. This study aims to improve our understanding of the role of dynamics, particularly the molecular movements that drive instabilities, through investigations of ASD made of Polyvinylpyrrolidone (PVP K12) and a model drug, Terfenadine. The analyses combine temperature modulated differential scanning calorimetry (MDSC) and dielectric relaxation spectroscopy. The results reveal that the produced ASDs are supersaturated with Terfenadine, regardless of the content, and that PVP slows down the dynamics of the blends, limiting the recrystallisation of the drug during heating. Although the ASDs appear homogeneous based on thermal analysis with a single glass transition consistently detected by MDSC, the investigation of the dynamics reveals a dissociation of the main relaxation into two components for PVP contents below 30 wt.%. This dynamic heterogeneity suggests a structural heterogeneity with the coexistence of two amorphous phases of different compositions, each characterised by its own dynamics. The complex evolution of these dynamics under recrystallisation is rationalised by the confrontation with the phase and state diagram of Terfenadine/PVP blends established by MDSC.

Formulation and Evaluation of Lumefantrine Solid Dispersions for Dissolution Enhancement

Lumefantrine (LUM) is a poorly water-soluble antimalarial drug that has limited bioavailability due to its low solubility and dissolution rate. The purpose of this study was to enhance the bioavailability of lumefantrine by preparing solid dispersions using polyvinylpyrrolidone K30 (PVP K30) as a hydrophilic carrier through the fusion method and solvent evaporation method. Solid dispersions (SDs) of LUM were prepared with varying drug-to-carrier ratios (1:1, 1:2, and 1:3) to optimize the formulation for enhanced dissolution properties. The solid dispersions were evaluated for their physicochemical properties, including morphology, drug content, solubility, in vitro dissolution and stability. Fourier-transform infrared (FTIR) spectroscopy also employed to analyze the possible interaction between LUM and PVP K30. The solubility and dissolution rate of lumefantrine were significantly enhanced in the solid dispersions compared to the pure drug. The formulation prepared by the solvent evaporation method showed the highest dissolution rate and solubility. The results demonstrate that the fusion method and solvent evaporation method are effective strategies for improving the solubility and bioavailability of lumefantrine, offering a promising approach for enhancing the therapeutic efficacy of this antimalarial drug.

Development and Evaluation of Polymeric Film Forming Solution of Ciclopirox Olamine for Topical Fungal Therapy

Aim: Formulation and assessment of polymeric film forming solution (PFFS) loaded with Ciclopirox olamine (CPO) for managing topical fungal infections. Methods: PFFS was prepared using a common solvent method with a range of polymers, such as Eudragit RL 100, Eudragit RS 100, PVP K30, PVP K90, HPC, HPMC K15, HPMC K4M, and PEG 400 in ethanol. The formulated PFFS was evaluated for Physicochemical properties, In vitro drug release, ex vivo permeation studies, stability studies, and antifungal assay. Results: The formulations have exhibited drying time of less than one minute. Most of them demonstrated uniform film formation, with an acceptable viscosity and pH within permissible limits, and with minimal outward stickiness. PFFS TR2 with CPO, Eudragit RL 100, and PEG 400 showed an In vitro drug release rate of 83.17% over 12 hours with controlled release kinetics. Ex vivo studies revealed a cumulative permeation of 1341.04 µg/cm² over 24 hours with a flux of 68.31 µg/cm²/hr, characterized by anomalous diffusion (non-Fickian transport), Moreover, the TR2 formulation achieved significant antifungal efficacy, with a zone of inhibition measuring 20±0.9 mm. Complementary characterization via FT-IR (Fourier Transform Infrared Spectroscopy) and DSC (Differential Scanning Calorimetry) confirmed the absence of drug-excipient interactions. Conclusion: The above study concludes that PFFS using Eudragit RL 100, Menthol: camphor, and PEG 400 showed enhanced antifungal activity and controlled release, suggesting it as a promising method for topical fungal treatment.

Formulation And Evaluation Of Metformin Hydrochloride Sustained Release Capsule

Metformin Hydrochloride (MH) is a synthesis of N, N -dimethyl guanidine, a type of medicament which is used to treat type II diabetes. Emil Worner and James Belt in the year 1922 were the first to synthesized dimethyl guanidine. MH has various other advantages such as; weight loss, improper fertility, slowing down the tumour growth and few more. The current work is focused on, to sustain the release of the drug in the body for a larger period of time. To perform this study various factor were taken into consideration such as drug, Excipients (HPMC, PVP K30, Magnesium stearate, MCC, NaCMC and Starch) compatibility study, Preformulation studies of raw material and granules. The granules were prepared using wet granulation method, and all the quality control parameter study for formulated 10 capsules were performed. Out of these 10 formulations, formulation 7 (F7) was subjected to have sustain release. Further, F7 was subjected to comparative study with other marketed available tablet and was found out that our formulation has sustained release up to the 13th hr and were as marketed tablet up to 11th hr. Finally accelerated stability study was performed till 3 months and was found that there were no significant changes.

Costunolide nanosuspension loaded in dissolvable microneedle arrays for atopic dermatitis treatment.

Costunolide nanosuspension loaded in dissolvable microneedle arrays for atopic dermatitis treatment.

Self-assembled metal-coordinated nanoparticles for synergistic energy metabolism inhibition and low-temperature photothermal therapy.

Self-assembled metal-coordinated nanoparticles for synergistic energy metabolism inhibition and low-temperature photothermal therapy.

Solubility and Dissolution Rate Enhancement of Bilastine by Solid Dispersion Technique

Bilastine (BLS) is non-sedating new-brand H1 antihistamine that has selective peripheral effects, the drug has a problem of an insufficient aqueous solubility and accordingly low dissolution rate, and low bioavailability. Solid dispersion (SD) is one of the most effective techniques for improving the solubility and the dissolution rate of poorly soluble drugs by the dispersion of drug within an inert hydrophilic carrier. The aim of this study is to increase the solubility and dissolution rate of the BLS using SD technique. Twenty-nine BLS SD formulas were prepared using different carrier polymers include Pluronic 407 (Poloxamer407), Poloxamer188, Urea, Polyethylene glycol 6000 (PEG6000) and Polyvinylpyrrolidone (PVP K30) and employing two different preparation methods (solvent evaporation and kneading method) at different drug: polymer ratios (1:1 ,1:3,1:5,1:10,1:15). The prepared SD formulas were evaluated for their percent yield, drug content, aqueous solubility, dissolution rate, PXRD, and FTIR. The SD technique successfully improved the solubility and dissolution rate of BLS. The improvement was largely dependent on the polymer type and drug: polymer ratio. The solubility improvement using different polymers was in the following order: PVP K30> PLX188> PEG6000> Urea> PLX407. The solid dispersion formula that showed the best outcomes in terms of dissolution improvement was prepared using the solvent evaporation technique employing PVP K30 at ratio of drug: polymer of 1:15. The optimized formula showed 10.2 folds increment in the solubility compared to pure BLS. It can be concluded that the SD technique can successfully improve the solubility and dissolution rate by solvent evaporation method with careful selection of the carrier polymer and drug: polymer ratio.

Design and formulation of fast-dissolving microneedles for the rapid transdermal delivery of lorazepam

This study investigates lorazepam-loaded dissolving microneedles (LMNs) as a fast-acting and minimally invasive treatment for status epilepticus. The LMNs were developed using a micro-moulding technique with an optimised combination of PVP K30, Dextran 40 and Pullulan. Their stability was confirmed through Fourier transform infra-red (FTIR) spectroscopy and X-ray diffraction (XRD) analysis. The Parafilm® membrane insertion test demonstrated 100% penetration efficiency, verifying their ability to effectively pierce the skin. Scanning electron microscopy (SEM) imaging revealed well-defined microneedles with precise dimensions (800 µm height, 200 µm base and 500 µm pitch). The LMNs rapidly dissolved in the subdermal layer of porcine skin. An ex vivo drug diffusion study showed that 3–5% of the encapsulated lorazepam was released within 30 min, with a cumulative release of 79.3% over 24 h. An acute dermal irritation study confirmed the biocompatibility and skin tolerance of the LMNs. Additionally, an in vivo anti-convulsant efficacy study in Albino Wistar rats subjected to maximal electroshock seizures demonstrated significant anticonvulsant effects (p < .05), confirming efficient systemic delivery of lorazepam. These findings highlight LMNs as a rapid-acting, non-invasive transdermal drug delivery system for managing status epilepticus, particularly in ambulatory care settings.

Development and Evaluation of Anti-Pollution Film-Forming Facial Spray Containing Coffee Cherry Pulp Extract.

Background/Objectives: This study aimed to develop and evaluate an anti-pollution film-forming spray (FFS) containing coffee cherry pulp extract (FFS-CCS). The formulation was designed to create a protective skin barrier, improving skin health while defending against environmental pollutants. Its physical properties, dust resistance, stability, skin penetration, and clinical effectiveness were assessed to ensure optimal performance and safety. Methods: Various polymers and a ternary solvent system were used to enhance the stability and solubility of bioactive compounds from the coffee cherry pulp extract. The formulations were characterized based on appearance, film formation, viscosity, pH, spray uniformity, spray pattern, angle, film thickness, and particle adhesion. Stability testing was conducted under different storage conditions. Skin penetration was assessed using Franz diffusion cells with Strat-M® membranes to simulate human skin. A single-blind, placebo-controlled trial with 42 participants was conducted over 60 days to evaluate the effects of FFS-CCS on skin hydration, tone, and wrinkle reduction. Clinical assessments were performed using a Corneometer, Mexameter, and Skin Visioscan. Results: The FFS1-CCS formulation, incorporating PVP K90 and a ternary solvent system, significantly improved the solubility, stability, and bioavailability of key bioactive compounds (chlorogenic acid, caffeine, and theophylline). Physical characterization confirmed uniform, transparent films with optimal viscosity and sprayability. Stability testing showed minimal degradation. Skin penetration and retention studies revealed enhanced retention of bioactive compounds with minimal systemic absorption. PVP K90, along with ethanol and propylene glycol, extended the compounds' residence time on the skin, ensuring localized delivery. Clinically, FFS1-CCS significantly improved skin hydration, reduced roughness, lightened skin tone, and decreased erythema. Conclusions: The FFS1-CCS formulation utilizing PVP K90 significantly enhanced the stability, bioavailability, and skin retention of coffee cherry pulp extract, resulting in improved skin hydration, wrinkle reduction, and skin tone enhancement. These findings highlight the potential of coffee cherry pulp extract as a multifunctional, sustainable cosmeceutical ingredient, offering both anti-aging and environmental protection benefits, making it a promising solution for skincare applications.

Development and Evaluation of Rivaroxaban Nanosus pension by Solvent Evaporation Method

Introduction: Medications that are not well soluble in water or both water and fat can be more effectively delivered with nanosuspension, as has been shown in previous studies. Traditional oral dosing forms can have their dosages reduced while still seeing improved absorption and bioavailability. Methods: A solvent evaporation method was employed to prepare a nanosuspension of rivaroxaban with the help of stabilizers such as PVP K30, PVA, poloxamer, and SLS. The revised formulation was found to have a zeta potential that falls within acceptable values. Nanosuspension formulations of Rivaroxaban were tested for goodness of fit using linear regression analysis, taking into account zero order and first-order kinetics as well as drug release equations. Results: The results showed that pure Rivaroxaban was poorly soluble in water (0.015 mg/ml) compared to other solvents, while it was more soluble in acetone. With an average particle size of 118 nm, the entrapment effectiveness varied between 82.15% and 97.31%. Researchers compared the drug release of commercially available formulation with that of manufactured nanosuspensions and found that the latter released more than 98% of the medication in just 60 minutes, while the former released just 79%. The findings of linear regression analysis using regression coefficients from the given data demonstrate that the improved formulation (F9) follows zero-order release kinetics. The strength of the Nanosuspension increased with an increase in polymer concentration, but the rate of medicine release dropped. Researchers using infrared spectroscopy found no evidence of drug-excipient interactions. Conclusion: F9 follows zero-order release kinetics and releases 99.84% of the medication in 25 minutes, making it the best formulation compared to the others.

Formulation and Characterization of Taste Mask Mouth Melt Film of Cetirizine HCl

The goal of the present study is to formulate and characterize taste mask mouth melt film containing cetirizine HCl to improve therapeutic efficacy by improving patient compliance and convenience for both younger and older patients. Varied batches of mouth melt films (MMF) of cetirizine HCl were prepared by the solvent casting process using varied quantities of HPMC K15, PVP K30, cross povidone, sodium starch glycolate, sucralose, orange flavour, aspartame citric acid used for increases salivation and colour also used. The films were assessed for physical appearance, weight variation, thickness, folding endurance, surface PH, drug content, disintegration time. The best formulation CTR6 exhibited acceptable folding endurance (150±1.03), least disintegration time (20±0.51 seconds), highest drug content (98.50±0.72mg) as compare to other formulation batches. The study concludes that formulation CTR6 of Mouth Melt Films for sublingual delivery of cetirizine HCl may be a best formulation than the other batches. The formulated batch can be a unique dosage form to better disintegration rate, beginning of action, and patient compliance. The best formulation (CTR6) yields satisfactory results.

Development and Evaluation of Therapeutically Beneficial Fast Dissolving Tablet Containing Herbal Extracts: A Quality by Design Approach

Objectives: The QbD approach validates the formulation during development, ensuring therapeutic benefits through the careful selection of herbal extracts. Methods: Oral dosage forms, especially fast dissolving tablets with different herbal extracts (curcumin, saffron, and gingerol) were developed to get their desired therapeutic actions immediately. Quality by Design (QbD) emphasizes a science-based approach to product development. Design of Experiments (DOE) and ANOVA are used to analyze high-risk Critical Quality Attributes (CQAs). Design Expert software helps determine the optimal quantities of variables in the formulation by analyzing the effects of independent variables to establish design space. Findings: The effect of identified independent variables croscarmellose sodium (CCS) and polyvinyl pyrrolidone K30 (PVP K30) were investigated. The impact of independent variables on critical responses Disintegration Time and Friability were analyzed. Both variables were found to have a sizeable impact on both the responses. The optimized formulation with 5mg/tablet of CCS and 0.5mg/tablet of PVP K30 meets the desired QTPP and Pharmacopoeial standards of fast dissolving tablet. ANOVA indicates the p-values of respective variables were 0.0168 and 0.0374 which indicates that the model was significant. The optimized FDT (fast dissolving tablet) formulation with three herbal combinations was found to have a DT of 22.02±0.83 seconds and hardness of 3.34±0.18 kg/cm² which was highly desired as per formulation perspectives. Novelty: The successful development of a fast-dissolving tablet with curcumin, saffron, and gingerol using a QbD approach highlights the unique challenges of formulation compared to other potent APIs. Moreover, achieving both the desired DT and hardness in a formulation with herbal extracts at 23.5% potency is a novel accomplishment. There is no existing QbD approach for a product that combines three different herbal extracts into a fast-dissolving tablet dosage form. Therefore, applying QbD to develop and optimize the formulation and achieve the desired results is an accomplishment. Keywords: Herbal Extracts, QbD - Quality By Design, Fast Dissolving Tablets, QTPP-Quality Target Product Profile, DOE-Design Of Experiments, CQA-Critical Quality Attributes