Formulation, Characterization and Release Behaviour of Metformin Hydrochloride Modified Release Tablet by Using Hydrophilic Polymers

Amongst the many public health problems, the diabetes mellitus is considered as a chronic life-style related disease which is now growing as an epidemic in both developed as well as developing countries. The current study is about formulation of metformin hydrochloride tablet to confirm their sustained release property by using various polymers. The tablets are prepared by granulation techniques using binding solution containing polyvinyl pyrolline K30. The possible interaction between the pure metformin hydrochloride and polymers are identified by Fourier transform-infrared spectroscopy. Tablets were formulated with different polymers like Hydroxy propyl methyl cellulose K100 and sodium carboxymethyl cellulose. Matrix prepared with high concentration of HPMC K100 polymer retards the drug release up to 6 h at 59 %, but the formulation 2 (F2) showed 72.72% of drug release in 6 h. The release of drug from the F2 formulation was found to be prolonged drug release when compared to other formulations. Hence our study conclude that the HPMC K100 polymer containing formulation showed good sustained release property owing to the high gel strength and well high viscosity nature of the polymer.

Formulation and Evaluation of Metoprolol Controlled Release Formulations

Aim: The main perspective of the present research work was to prepare Metoprolol floating controlled release formulations. Methodology: After performing the characterization studies, Metoprolol tablets were prepared using various concentrations of poly ethylene oxide (PEO) WSR 303 (5% to 30%) by direct compression method. Formulations MP1 and MP6 were formulated using PEO WSR 303. Various pre and post compression parameters were evaluated. Dissolution studies were performed for the prepared tablets using dissolution medium of 0.1N hydrochloric acid. Results: Characterization studies like Fourier Transform Infra Red (FTIR) and Scanning Electron Microscopy (SEM) for Metoprolol, Polyethylene oxide WSR 303 and their combination were carried out, which revealed that there is no interaction between drug and polymer. The dissolution studies showed the controlled release pattern of Metoprolol up to 24h. The formulation MP5 prepared using 25% w/w of PEO WSR 303 showed maximum drug release of 98.22% at 24h. Similar drug release profile was observed for MP6 which was formulated using 30%w/w PEO WSR 303. These two formulations were further added with various concentrations of sodium bicarbonate (5% to 15%) and citric acid (2.5% to 10%) which enhanced floating of drug. Formulation MP8 containing 10% of sodium bicarbonate with 25% PEO WSR 303 showed less buoyancy lag time and prolonged drug release. Formulation MP15 showed very less buoyancy lag time of 4sec. Conclusion: Thus the prepared Metoprolol floating tablets showed prolonged drug release which could be a promising formulation for anti-hypertensive patients.

Sorafenib Repurposing for Ophthalmic Delivery by Lipid Nanoparticles: A Preliminary Study

Uveal melanoma is the second most common melanoma and the most common intraocular malignant tumour of the eye. Among various treatments currently studied, Sorafenib was also proposed as a promising drug, often administered with other compounds in order to avoid resistance mechanisms. Despite its promising cellular activities, the use of Sorafenib by oral administration is limited by its severe side effects and the difficulty to reach the target. The encapsulation into drug delivery systems represents an interesting strategy to overcome these limits. In this study, different lipid nanoparticulate formulations were prepared and compared in order to select the most suitable for the encapsulation of Sorafenib. In particular, two solid lipids (Softisan or Suppocire) at different concentrations were used to produce solid lipid nanoparticles, demonstrating that higher amounts were able to achieve smaller particle sizes, higher homogeneity, and longer physical stability. The selected formulations, which demonstrated to be biocompatible on Statens Seruminstitut Rabbit Cornea cells, were modified to improve their mucoadhesion, evaluating the effect of two monovalent cationic lipids with two lipophilic chains. Sorafenib encapsulation allowed obtaining a sustained and prolonged drug release, thus confirming the potential use of the developed strategy to topically administer Sorafenib in the treatment of uveal melanoma.

Preparation and Evaluation of Captopril Oral Floating Controlled Release Formulations

Aim: Dosing frequency is a major hurdle in geriatrics with frequent drug administration. In such cases, oral controlled release floating formulations are helpful which causes reduction in dosing frequency and fluctuation of drug levels in plasma. The main aim of the current research was to prepare Captopril floating controlled release formulations in order to achieve extended gastric retention in the upper GIT. Methodology: Captopril tablets were prepared using different concentrations of poly ethylene oxide water soluble resin (PEO WSR) 303 (5% to 30%) by direct compression technique. Captopril formulations CSP1 and CSP6 were formulated using PEO WSR 303. Pre and post compression parameters were evaluated. Dissolution studies were performed for the prepared tablets using 0.1N hydrochloric acid as dissolution medium. Results: The dissolution studies showed controlled drug release up to 12h. The formulation CSP5 prepared using 25% w/w of PEO WSR 303 showed maximum drug release of 97.97% at 12h. Almost similar drug release profile was also observed for CSP6 which was prepared using 30%w/w PEO WSR 303. These two formulations were further added with various concentrations of sodium bicarbonate (5% to 15%) and citric acid (2.5% to 10%) which enhanced floating of drug in Gastro intestinal tract (GIT). Formulation CSP8 containing 10% of sodium bicarbonate with 25% PEO WSR 303 showed less buoyancy lag time and prolonged drug release. Formulation CSP15 showed very less buoyancy lag time of 5sec. Characterization studies like Fourier Transform Infra Red spectroscopy (FTIR) and Scanning Electron Microscopy (SEM) were also carried out. Conclusion: The prepared Captopril floating tablets could be an alternative formulation for prolonged drug release.

Thermosensitive Interfacial Migration of 5-FU in the Microenvironment of Pluronic Block Copolymers

Chemotherapy is one of the most important ways to treat cancer. At present, chemotherapy medicines are mainly administered by intravenous injection or oral administration. However, systemic medical care requires the dosage of high concentrations of drugs to defeat the malignant tumor growth. In recent years, the use of polymer composites for local and sustained drug release has become an important field of research to minimize side effects due to high-concentration chemotherapy drugs. Here, 19F-{1H} heteronuclear Overhauser enhancement spectroscopy (HOESY) was used to study the micellular environment of the F-containing chemotherapeutic drug 5-FU in Pluronic F127, Pluronic L121, and F127/L121 binary blending composites. The distribution of 5-FU in micelles is related to the PEO and PPO segment length of Pluronic polymers and the environmental temperature. The drug release tests further confirm that if 5-FU medicines were loaded in the PPO segment inside the micelles, the purpose of the prolonged drug release carrier is achieved.

Aspirin-Loaded Polymeric Films for Drug Delivery Systems: Comparison between Soaking and Supercritical CO2 Impregnation

Polymeric implants loaded with drugs can overcome the disadvantages of oral or injection drug administration and deliver the drug locally. Several methods can load drugs into polymers. Herein, soaking and supercritical CO2 (scCO2) impregnation methods were employed to load aspirin into poly(l-lactic acid) (PLLA) and linear low-density polyethylene (LLDPE). Higher drug loadings (DL) were achieved with scCO2 impregnation compared to soaking and in a shorter time (3.4 ± 0.8 vs. 1.3 ± 0.4% for PLLA; and 0.4 ± 0.5 vs. 0.6 ± 0.5% for LLDPE), due to the higher swelling capacity of CO2. The higher affinity of aspirin explained the higher DL in PLLA than in LLDPE. Residual solvent was detected in LLDPE prepared by soaking, but within the FDA concentration limits. The solvents used in both methods acted as plasticizers and increased PLLA crystallinity. PLLA impregnated with aspirin exhibited faster hydrolysis in vitro due to the catalytic effect of aspirin. Finally, PLLA impregnated by soaking showed a burst release because of aspirin crystals on the PLLA surface, and released 100% of aspirin within 60 days, whereas the PLLA prepared with scCO2 released 60% after 74 days by diffusion and PLLA erosion. Hence, the scCO2 impregnation method is adequate for higher aspirin loadings and prolonged drug release.

Fabrication of Non-phospholipid Liposomal Nanocarrier for Sustained-Release of the Fungicide Cymoxanil

Liposome nanocarriers can be used to solve problems of pesticide instability, rapid degradation and a short period of efficacy. Cymoxanil with antifungal activity requires an ideal drug loading system due to its degradation issues. In this paper, cholesterol and stearylamine were used to prepare non-phospholipid liposomes (sterosomes) as a pesticide nanocarrier, and were characterized with field emission scanning electron microscopy (FE-SEM), X-ray powder diffraction (XRD), Fourier-transform infrared (FT-IR) spectrometer, size distribution, and ζ-potential. The results showed sterosomes were successfully loaded with cymoxanil. The loading efficiency and the drug-to-lipid ratio were 92.6% and 0.0761, respectively. Prolonged drug release was obtained for 3 days, improving the short duration of the drug itself. The addition of cymoxanil-loaded sterosomes in culture medium effectively inhibited the growth of yeast cells, which serve as model fungal targets. Sterosomes as nanocarriers significantly improved the stability and efficacy of cymoxanil, thus introducing practical and economically desirable strategies for the preparation of novel pesticide formulations.

Encapsulation of Opiorphin in Polymer-coated Alginate Beads for Controlled Delivery and Painkilling

Opiorphin (Oph) is a naturally produced endogenous peptide with a strong analgesic effect, superior to that of morphine, and without the severe side effects that morphine and morphine-like drugs exert. However, despite its strong therapeutic potential, the short duration of action, probably due to its low chemical stability and rapid degradation by the peptidases in the bloodstream, represents a serious obstacle to the Oph use into clinical practice. In this work a novel approach to construct Oph-loaded particles as a platform for its delivery has been developed. Gel beads loaded with Oph were synthesized from alginate, a naturally occurring biodegradable anionic polysaccharide, and coated with polyelectrolyte multilayers (from natural polyelectrolytes (chitosan and hyaluronic acid) and synthetic polyelectrolytes (poly(allylamine hydrochloride) and poly(styrene sulfonate)) or hybrid polyelectrolyte-graphene oxide multilayers. All coated Oph-loaded alginate beads show prolonged drug release compared to the non-coated ones, but the extent of the prolongation depends on the type of the coating. We expect that the successful encapsulation of opiorphin in biodegradable particles will provide an opportunity for the development of adequate drug delivery system with effective and prolonged analgesic activity and will offer a new alternative for pain management.

Incorporation of Fluconazole and Ocimum Sanctum Oil in Soft Denture Liners to Treat Biofilms of Candida albicans Associated with Denture Stomatitis

Purpose: To investigate the In Vitro activity of incorporated antifungal agents like Fluconazole and Ocimum sanctum oil (Tulsi) in the denture soft liners to reduce the risks associated with the biofilms of Candida albicans.Materials and Methods: In the current study, the minimum inhibitory concentration (MIC) of two antifungal agents namely Fluconazole and O. sanctum (Tulsi oil) against C. albicans (ATCC 10231) was evaluated to examine their effect in reducing the count of candida and its biofilms. Analysis of physical properties such as surface roughness and hardness of soft denture liners (test and control) were also performed. The effect of both antifungal agents was also observed on cell morphology of candida cells using scanning electron microscopy (SEM).Results: Studies confirmed MIC value for fluconazole and O. sanctum oil as 600 and 400 µg/ml respectively. Surface hardness and roughness of soft denture material (test) remained unaltered. Finally, SEM studies also proved the effectiveness of incorporated antifungal agents on the cell morphology of C. albicans at their respective MIC values.Conclusions: This approach allows the prolonged drug release in the oral cavity which simultaneously treats the injured denture bearing tissues and also the infection, biofilms of candida without compromising on their physical properties. These studies are significant and have tremendous medicinal and therapeutic relevance.