Tyrosinase inhibitor-loaded microsponge drug delivery system: new approach for hyperpigmentation disorders.

OBJECTIVE: The aim of the present investigation was to design and formulate appropriate form of glabridin, using microsponge drug delivery system. METHOD: Microsponges were prepared by emulsion solvent evaporation method and characterized by drug loading, infrared spectroscopy and scanning electron microscopy. In vitro diffusion studies of gel formulation were performed using ethanol: phosphate buffer (1:1) mixture as receptor medium. Animal studies were carried out using brownish guinea pigs with UV-induced pigmentation model. RESULTS: Prepared microsponges were predominantly yellowish, free-flowing and spherical in shape. The infrared spectra revealed the absence of drug polymer interaction. Scanning electron microscopy (SEM) and porosity studies confirmed spherical and porous nature. In vitro release studies data depicted highest correlation with Higuchi treatment. Animal studies also supported the better depigmenting activity as compared to plain gel. CONCLUSION: Glabridin microsponge-loaded gel could be efficacious in treating various hyperpigmentation disorders.

Designing of the mucoadhesive intravaginal spermicidal films.

A mucoadhesive drug delivery system for local delivery of metronidazole through vaginal route was formulated. Films were prepared by solvent evaporation method using various compositions of Carbopol, hydroxypropylmethylcellulose, chitosan, Polyox and propylene glycol. The films were evaluated for their weight, thickness, surface pH, folding endurance, mechanical, drug content uniformity, in vitro drug release, swelling, gelling and mucoadhesion property. All the films possess satisfactory film characteristics. Films made of Polyox found to possess acceptable, physicochemical, mechanical, gelling and mucoadhesion property for delivery of metronidazole.

Development and characterization of mucoadhesive buccal patches of salbutamol sulphate.

Mucoadhesive patch releasing the drug in the oral cavity at predetermined rate may present distinct advantages over traditional dosage forms such as tablets, gels and solutions. The present study was concerned with the preparation and evaluation of mucoadhesive buccal patches for the controlled systemic delivery of Salbutamol sulphate to avoid first pass hepatic metabolism. The developed patches were evaluated for the physicochemical, mechanical and drug release characteristics. The patches showed desired mechanical and physicochemical properties to withstand environment of oral cavity. The in-vitro release study showed that patches could deliver drug to the oral mucosa for a period of 7 h. the patches exhibited adequate stability when tested under accelerated conditions.

Update on nonoxynol-9 as vaginal spermicide.

Nonoxynol-9 (N-9) is a typical surfactant. For more than 30 years that very property of N-9 has been successfully exploited for its spermicidal action. It is available as an over-the-counter, locally acting vaginal spermicide. The suitability of N-9 as a spermicide is elaborated in this article. The reasons why N-9 may fail as a contraceptive are discussed. In spite of many drawbacks, which are mentioned in the article, N-9 is still often resorted to as a locally acting contraceptive. The review ends with suggestions to alter the molecular structure of N-9 and to adjust the dosages.

Sintering of wax for controlling release from pellets.

The purpose of the present study was to investigate incorporation of hydrophobic (ie, waxy) material into pellets using a thermal sintering technique and to evaluate the pellets in vitro for controlled release. Pellets prepared by extrusion-spheronization technology were formulated with a water-soluble drug, microcrystalline cellulose, and carnauba wax. Powdered carnauba wax (4%-20%) prepared by grinding or by emulsification was studied with an attempt to retard the drug release. The inclusion of ground or emulsified carnauba wax did not sustain the release of theophylline for more than 3 hours. Matrix pellets of theophylline prepared with various concentrations of carnauba wax were sintered thermally at various times and temperatures. In vitro drug release profiles indicated an increase in drug release retardation with increasing carnauba wax concentration. Pellets prepared with ground wax showed a higher standard deviation than did those prepared with emulsified wax. There was incomplete release at the end of 12 hours for pellets prepared with 20% ground or emulsified wax. The sintering temperature and duration were optimized to allow for a sustained release lasting at least 12 hours. The optimized temperature and duration were found to be 100 degrees C and 140 seconds, respectively. The sintered pellets had a higher hydrophobicity than did the unsintered pellets. Scanning electron micrographs indicated that the carnauba wax moved internally, thereby increasing the surface area of wax within the pellets.

A flexible technology for modified release of drugs: multi layered tablets.

Modified release dosage forms offer definite advantages over conventional release formulation of the same drug. Hydrophilic polymers are mainly used for preparation of matrix type controlled delivery systems. The system usually provides nonlinear release profile. The multi-layered matrix system overcomes inherent disadvantages of non-linearity associated with diffusion controlled matrix devices by providing additional release surface with time to compensate for the decreasing release rate. This technology also demonstrates a wide flexibility for various applications. In this article, we review system design, various constructions and formulation parameters of modified release dosage forms.