Development And Evaluation Of Taste Masked Orally Disintegrating Tablets Of A Water Soluble Drug, Sumatriptan Succinate And A Water Insoluble Drug, Ondansetron

The aim of the present research was to formulate taste masked orally disintegrating tablets (ODTs) of ondansetron (water insoluble) and sumatriptan succinate (water soluble) using different available technologies namely Orasolv, freeze drying and Wowtab. In Wowtab and freeze drying techniques, the bitter taste of ondansetron was masked by the addition of a sweetener (aspartame), whereas in the Orasolv technique by complexing the drug with Eudragit EPO (1:0.5). In all the techniques used to prepare sumatriptan succinate ODTs, the intensely bitter taste of the drug was masked by coating it with Eudragit EPO (1:1) using spray dryer

Formulation and characterization of pH induced in situ gels containing sulfacetamide sodium for ocular drug delivery: A combination of Carbopol^®/HPMC polymer

© 2019, Association of Pharmaceutical Teachers of India. All rights reserved. Introduction: Topical delivery of eye drops which currently accounts to 90% of available ocular dosage forms are ideal for the treatment of eye diseases but having limitations of poor therapeutic response and low bioavailability. Objectives: The objectives of present research was to develop and characterize sustained release in situ ocular gels containing sufacetamide sodium using pH induced gelling polymers for improved therapeutic response and patient compliance. Methods: In situ gel formulations prepared by dispersion method using Carbopol® 940/Carbopol® 934 alone or in combination with hydroxypropyl methylcellulose (HPMC E4M). Formultaions were evaluated for appearance, pH, viscosity, gelling capacity, drug content and in vitro drug release. The optimized formulation was assessed for sterility and antimicrobial efficacy using disk diffusion technique in comparison to commercial eye drops (Albucid®10%). Results: The appearance of in situ gels were clear and free flowing in nature however, a viscous clear solution with no flow was produced for formulations consisting of 0.8% w/v Carbopol® 940/Carbopol® 934 and 2% w/v HPMC E4M. pH of all the formulations was within the range of 5.9 to 6.7. In situ gels with Carbopol® 940 demonstrated higher viscosity compared to Carbopol® 934 and drug release was sustained over a period of 8 hr. The selected formulation containing 0.8% w/v Carbopol® 940 and 1.5% w/v HPMC E4M passed sterility test and demonstrated similar antimicrobial efficiency compared to commercial product. Conclusion: Carbopol®/HPMC-based in situ gels have potential to improve patient’s compliance by reducing the dosing frequency and could be a viable alternative to commercial product

Preparation and in vitro characterization of non-effervescent floating drug delivery system of poorly soluble drug, carvedilol phosphate

The objective of the study was to enhance the solubility of carvedilol phosphate and to formulate it into non-effervescent floating tablets using swellable polymers. Solid dispersions (SD)of carvedilol were prepared with hydrophilic carriers such as polyvinylpyrrolidone and poloxamer to enhance solubility. Non-effervescent floating tablets were prepared with a combination of optimized solid dispersions and release retarding polymers/swellable polymers such as xanthan gum and polyethylene oxide. Tablets were evaluated for physicochemical properties such as hardness, thickness and buoyancy. SD prepared with the drug to poloxamer ratio of 1:4 by melt granulation showed higher dissolution rate than all other dispersions. Formulations containing 40 mg of polyethylene oxide (C-P40) and 50 mg xanthan gum (C-X50) were found to be best, with the drug retardation up to 12 hours. Optimized formulations were characterized using FTIR and DSC and no drug and excipient interactions were detected

Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG

YesThe aim of this study was to design a controlled release vehicle for insulin to preserve its stability and biological activity during fabrication and release. A modified, double emulsion, solvent evaporation, technique using homogenisation force optimised entrapment efficiency of insulin into biodegradable nanoparticles (NP) prepared from poly (dl-lactic-co-glycolic acid) (PLGA) and its PEGylated diblock copolymers. Formulation parameters (type of polymer and its concentration, stabiliser concentration and volume of internal aqueous phase) and physicochemical characteristics (size, zeta potential, encapsulation efficiency, in vitro release profiles and in vitro stability) were investigated. In vivo insulin sensitivity was tested by diet-induced type II diabetic mice. Bioactivity of insulin was studied using Swiss TO mice with streptozotocin-induced type I diabetic profile. Insulin-loaded NP were spherical and negatively charged with an average diameter of 200–400 nm. Insulin encapsulation efficiency increased significantly with increasing ratio of co-polymeric PEG. The internal aqueous phase volume had a significant impact on encapsulation efficiency, initial burst release and NP size. Optimised insulin NP formulated from 10% PEG–PLGA retained insulin integrity in vitro, insulin sensitivity in vivo and induced a sustained hypoglycaemic effect from 3 h to 6 days in type I diabetic mice

Molecular modulators of celastrol as the keystones for its diverse pharmacological activities

© 2018 The Authors In the recent years, much attention has been focused on identifying bioactive compounds from medicinal plants that could be employed in therapeutics, which is attributed to their potent pharmacological actions and better toxicological profile. One such example that has come into the light with considerable interest is the pentacyclic triterpenoid, celastrol, which has been found to provide substantial therapeutic properties in a variety of diseases. In an effort to further accelerate its potential to be utilized in clinical practice in the future; along with advancing technologies in the field of drug discovery and development, different researchers have been investigating on the various mechanisms and immunological targets of celastrol that underlie its broad spectrum of pharmacological properties. In this review, we have collated the various research findings related to the molecular modulators responsible for different pharmacological activities shown by celastrol. Our review will be of interest to the herbal, biological, molecular scientist and by providing a quick snapshot about celastrol giving a new direction in the area of herbal drug discovery and development

Formulation, characterization, in vitro, in vivo, and histopathological evaluation of transdermal drug delivery containing norfloxacin and Curcuma longa.

OBJECTIVE: In an attempt for better treatment of bacterial infections and burn wounds, semisolid formulations containing norfloxacin (NF) and natural wound healing agent Curcuma longa were prepared. The rationale behind employing combination of NF and Curcuma longa is to obtain synergistic wound healing effect. The prepared formulations were compared with silver sulfadiazine cream 1%, USP. MATERIALS AND METHODS: Various ointments containing NF and C. longa were prepared using standard procedures. These formulations were evaluated for antimicrobial activity against various strains of aerobic and anaerobic microorganisms. The wound healing property was evaluated by histopathological examination and by measuring the wound contraction. RESULTS: The significant antimicrobial and wound healing effects were demonstrated by formulations which are comparable with silver sulfadiazine 1% cream (P < 0.05). Various morphological changes were observed by histopathology during the study period (days 1, 4, 8, and 12) which also supported the wound healing process. CONCLUSION: Based on the observed antimicrobial and wound healing effects, the formulations containing combination of NF and Curcuma longa could be employed as an alternative to commercial silver sulfadiazine 1% cream. This innovative mode of formulation can be employed for making burn wound healing process more effective