Hydroxypropyl Methylcellulose E50 Research Articles

Fabrication and Characterization of Dissolving Microneedles Containing Oryza sativa L. Extract Complex for Enhancement of Transfollicular Delivery.

Dissolving microneedles are extensively applied in drug delivery systems to enhance penetration into the skin. In this study, dissolving microneedles fabricated from polyvinylpyrrolidone K90 (PVP-K90) and hydroxypropylmethyl cellulose (HPMC) E50 in different ratios were characterized. The selected formulations incorporated Oryza sativa L. extract complex and its characteristics, transfollicular penetration, and safety were observed. The microneedles, fabricated from PVP K90: HPMC E50 in a ratio of 25:5 (P25H5) and 20:10 (P20H10), revealed excellent morphological structure, proper mechanical strength, and excellent skin insertion. P25H5 microneedles exhibited faster dissolution than P20H10 microneedles. Microneedles containing Oryza sativa L. extract complex showed excellent morphological structure via scanning electron microscopy but decreased mechanical strength. P25H5-O, which exhibited an effective ability to enter skin, was selected for further investigation. This microneedle formulation had a high percentage of drug-loading content, enhanced skin penetration via the transfollicular route, and was safe for keratinocytes. As a result, the dissolving microneedle containing Oryza sativa L. extract complex can be used to enhance transfollicular delivery through the skin with safety.

Enhanced dissolution of curcumin-resorcinol cocrystal by the inhibition effect of HPMCAS on solution-mediated phase transformation

The present study aimed to investigate the inhibition effect of polymers on the solution-mediated phase transformation (SMPT) of cocrystals during dissolution. Curcumin-resorcinol (CUR-RES) cocrystal was prepared by slow solvent evaporation, and the best precipitation inhibitor of curcumin (CUR) was selected from five polymers including hydroxypropyl methylcellulose acetate succinate (HPMCAS), hydroxypropyl methylcellulose (HPMC) E5, HPMC E50, Poloxamer 188 (P188) and polyethylene glycol (PEG) 6000 by solvent-shift precipitation test. Then non-sink dissolution tests and intrinsic dissolution rate (IDR) tests were performed with or without HPMCAS to explore the influence of HPMCAS on the dissolution of the cocrystal. It was showed that HPMCAS could effectively inhibit the crystallization of CUR so that the dissolved drug concentration in a predissolved 0.1 % HPMCAS solution at 2 h was nearly 15 μg/mL, which was at least 150 times higher than that without HPMCAS. The red CUR-RES cocrystal turned gradually to yellow CUR during the dissolution tests in the absence of HPMCAS, while the transformation was prevented in the presence of HPMCAS. The present work fully exploits the solubility advantages of CUR-RES cocrystal via the use of precipitation inhibitor and offers important insights into reducing the risk of SMPT during cocrystal dissolution, which is crucial for the development of pharmaceutical cocrystal formulations.

Development and characterization of bimodal chrono modulated drug delivery of methylphenidate hydrochloride

The study's goal was to develop chrono modulated pulsatile tablets of methylphenidate hydrochloride with an extended-release pattern in the morning and an immediate burst release in the afternoon for exaggerated symptoms of attention deficit hyperactivity disorder match the circadian rhythm of disease, where high levels of l-3, 4-dihydroxyphenylalanine (DOPA) are observed in the afternoon, necessitating higher drug concentrations. The core tablets were made with Kollidon CL-SF as a super disintegrant at 4% and 8% concentrations, with microcrystalline cellulose PH 102 (Pharma grade) and Ludipress as diluents.The core tablets were then compress coated with a slow-release component blend containing different grades of hydroxypropyl methylcellulose (HPMC) at various concentrations of HPMC E50, HPMC E15M, or HPMC E4M, as well as 4% Ethocel. Among all formulations, the F10 formulation containing HPMC E50 at 70% showed the best drug release, with 60% of the dose released slowly over 4 h, followed by an immediate burst of the remaining 40% at the 5th hour. The effect of different diluents on in vitro drug release kinetics and in vitro dissolution studies were performed for all formulations, and A1 formulation containing Cellactose-80 as a diluent showed the best results, with results matching the circadian variations in the disease condition.

Fast-dissolving oral films containing dextromethorphan/phenylephrine for sinusitis treatment: formulation, characterization and optimization.

This work uses optimization study to formulate a patient-friendly antitussive fast-dissolving oral film based on phenylephrine hydrochloride (Phen) and dextromethorphan hydrobromide (Dex). The designed films were based on hydroxypropylmethyl cellulose (HPMC) with two grades (E5 and E50) as a film-forming polymer by the solvent-casting method. Polyethylene glycol with two molar masses (400 and 1000) was used as a plasticizer, while aspartame was used as a sweetener and microcrystalline cellulose intended to act as a disintegrant. To find an optimum formulation, a response surface methodology and a central composite design were employed. The percentage of HPMC E50, and PEG, as a plasticizer, were considered to be the design factors. Film thickness, surface pH, disintegration time, dissolution percent, tensile strength, elongation percent and folding endurance were considered to be the responses. A film with 11.46% E50, 88.54% E5, 25% of two drugs (8.4% of Phen and 16.6% of Dex) and 18.54% plasticizer is designed and prepared as the optimum formulation for Phen/Dex fast-dissolving oral films, with 95% confidence levels.

Characterization of Hydrophilic Polymers as a Syringe Extrusion 3D Printing Material for Orodispersible Film.

The application of hydrophilic polymers in designing and three-dimensional (3D) printing of pharmaceutical products in various dosage forms has recently been paid much attention. Use of hydrophilic polymers and syringe extrusion 3D printing technology in the fabrication of orodispersible films (ODFs) might hold great potential in rapid drug delivery, personalized medicine, and manufacturing time savings. In this study, the feasibility of 3D-printed ODFs fabrication through a syringe extrusion 3D printing technique and using five different hydrophilic polymers (e.g., hydroxypropyl methylcellulose E15, hydroxypropyl methylcellulose E50, high methoxyl pectin, sodium carboxymethylcellulose, and hydroxyethylcellulose) as film-forming polymers and printing materials has been investigated. Rheology properties and printability of printing gels and physicochemical and mechanical properties of 3D-printed ODFs were evaluated. Amongst the investigated hydrophilic polymers, sodium carboxymethylcellulose at a concentration of 5% w/v (SCMC-5) showed promising results with a good printing resolution and accurate dimensions of the 3D-printed ODFs. In addition, SCMC-5 3D-printed ODFs exhibited the fastest disintegration time within 3 s due to high wettability, roughness and porosity on the surface. However, the results of the mechanical properties study showed that SCMC-5 3D printed ODFs were rigid and brittle, thus requiring special packaging to prevent them from any damage before practical use.

Therapeutic Efficacy of Moxifloxacin Mucoadhesive Hydrogel for Bacterial Keratitis

Bacterial keratitis is a hypothetically devastating corneal infection due to the opportunity of fast development; corneal devastation either to be completed in 24–48 hours with even more contagious bacterial aetiological agents. Moxifloxacin mucoadhesive Hydrogel was prepared by using polymer Hydroxy Propyl Methyl Cellulose E50 LV by hydration method. Moxifloxacin was dissolved in small quantity of water and Benzalkonium Chloride was added to the Polymer solution. The formulations were evaluated for clarity, pH measurement, spread-ability test, drug content estimation, viscosity study, in vitro diffusion study and antibacterial activity. The developed formulation exhibits the sustained release over a period of 10 hour. The optimized formulation was further evaluated with antimicrobial activity. The results of the in-vitro antimicrobial activity of hydrogel were satisfactory.
 Keywords: Corneal Infection, Hydrogel, Moxifloxacin, invitro release

Surface Tracking of Curcumin Amorphous Solid Dispersions Formulated by Binary Polymers

Herein, curcumin amorphous solid dispersions (Cur ASDs) were prepared using binary polymers (Eudragit EPO with polyvinylpyrrolidone K30 [EuD-PVP], Eudragit EPO with hydroxypropyl methylcellulose E50 [EuD-HPMC]) as excipient, and surface tracking of Cur ASDs was mainly addressed. Infrared spectroscopy, in situ Raman imaging spectroscopy, molecular docking modeling, and contact angle measurements were mainly applied to study the molecular interaction and wetting property of Cur ASDs. Cur/EuD-PVP had a lower cumulative release (approximately 15%) than Cur/EuD-HPMC (approximately 48%) because Cur/EuD-HPMC presented carrier-controlled wetting property while Cur/EuD-PVP fitted to a drug-controlled wetting property. The favorable HPMC can be preferred as superior excipient for Cur ASDs compared with binary polymers, which has potential application in food and drug healthcare industry of Cur.

Design of a Time-Controlled Pulsatile Release System for Propranolol Using the Dry-Coated Method: In Vitro and In Vivo Evaluation.

The objective of this study was to design a time-controlled pulsatile release (TCPR) system containing propranolol (PNH) as an active pharmaceutical ingredient. Here, the developed dosage forms were coated with hydroxypropyl-methylcellulose (HPMC) and other excipients as barrier layer using dry-coated technology. The influence of HPMC, microcrystalline cellulose (MCC), and lactose in the outer coating and the coating weight on drug release were investigated. Then, a three-factor, five-level central composite design (CCD) and response surface method were used to optimize the formula of the coating. After data processing, the optimal prescription was found to be as follows: HPMC E50(X1) 86.2mg, MCC(X2) 43.8mg, and lactose (X3) 21.3mg in the coating. Moreover, the in vitro tests showed that the optimized formulation of TCPR had a lag time of 4h followed by a 4-h drug release. Also, determination of the extent of erosion of the TCPR tablets revealed that the lag time is related to the coating erosion speed. The in vivo test in beagle dogs and comparison of the parameters for the TCPR tablets and reference preparations showed significant differences for Tmax (7.83±0.408 and 2±0.00) and Cmax (185.45±28.561 and 587±45.27ng/ml) but no significant differences in the AUC0-∞ (1757.876±208.832 and 1779.69±229.02ng h/ml). These results demonstrated that the TCPR tablets successfully prolonged the lag time and controlled the release of propranolol.

Preparation and characterization of dipyridamole solid dispersions for stabilization of supersaturation: effect of precipitation inhibitors type and molecular weight

Dipyridamole (DPL) is a weakly basic BCS class II drug which precipitates upon entering into intestine leading to pH dependant and variable absorption. Thus, research envisaged focuses on developing formulations that maintain supersaturation following upon acid to neutral pH transition. In an endeavor to accomplish the objective, solid dispersion (SD) with hydroxypropylmethyl cellulose (HPMC) and polyvinylpyrrolidone (PVP) was prepared by a quench cooling method. The three molecular weight grades of HPMC (HPMC E5, HPMC E15 and HPMC E50) and two molecular weight grades of PVP (PVP K30 and PVP K90) were investigated to observe effect of increasing molecular weight on stabilizing DPL supersaturated solutions. Equilibrium solubility studies revealed increase in solubility with both HPMC and PVP with greater benefit from HPMC. In vitro supersaturated dissolution results demonstrated that HPMC formulations provided greater degree and extent of supersaturation as compared to PVP formulations. The formulation with HPMC E50 provided maximum stabilization to supersaturation upon acid to neutral pH transition. Moreover, the effect of increase in molecular weight was more pronounced in HPMC rather than PVP. Stronger interactions were observed for DPL with HPMC, while no interaction was observed with PVP which was evident from Fourier transform infra-red studies. Differential scanning calorimetry and powder X-ray diffraction studies revealed the amorphous state of DPL in SD.

Fabrication and in vitro evaluation of bidirectional release and stability studies of mucoadhesive donut-shaped captopril tablets

Objective: To obtain controlled release of captopril in the stomach, coated, mucoadhesive donut-shaped tablets were designed.Materials and methods: Donut-shaped tablet were made of different ratios of diluents to polymer or combination of polymers by direct compression method. Top and bottom portions of the tablet were coated with water-insoluble polymer followed by mucoadhesive coating. Time of water penetration, measurement of tensile strength, mucoadhesion studies (static ex vivo and ex vivo wash-off) were taken into account for characterization of respective films. In vitro study has been performed at different dissolution mediums. Optimized batches were also prepared by wet granulation. Stability studies of optimized batches have been performed.Results: The results of time of water penetration and tensile strength indicated positive response against water impermeation. Mucoadhesive studies showed that film thickness of 0.12 mm was good for retention of tablet at stomach. At pH 1.2, optimized batch of tablet made with hydroxypropyl methyl cellulose (HPMC) E15 as binder showed 80% w/w drug release within 4–5 h with maximum average release of 97.49% w/w. Similarly, maximum average releases of 96.36% w/w and 95.47% w/w were obtained with nearly same dissolution patterns using combination of HPMC E5 and HPMC E50 and sodium salt of carboxy methyl cellulose (NaCMC) 500–600 cPs instead of HPMC E15. The release profiles in the distilled water and pH 4.5 followed the above pattern except deviation at pH 6.8. Stability studies were not positive for all combinations.Conclusion: Coated, mucoadhesive donut-shaped tablet is good for controlled release of drug in the stomach.