orabase and Heart-Failure

Due to changing lifestyles of modern world, cardiac failures are increasing day by day. Drug delivery systems that can overcome the drawbacks of conventional drug administration are highly desired. Diltiazem hydrochloride (DTZ) is a common and effective drug used for cardiac failures. However, its efficient loading, high bio availability and sustained transdermal release from polymer matrix are of high demand. Herein, the main objective was to fabricate a transdermal drug delivery system (TDDS) capable of efficient DTZ loading with sustained release. Owing to the high hydrophilicity of DTZ, a hydrophilic matrix comprising of poly ethylene glycol coated vinyl trimethoxy silane-g-chitosan (PEG@VTMS-g-CS) was developed. DTZ encapsulated copolymer was dispersed in matrices like sodium alginate (ALG), carboxy methyl cellulose (CMC) and poly vinyl alcohol (PVA). Economic viability and cosmetic attractiveness of the films were evaluated and optimum results were obtained for PVA matrix. The in vitro skin penetration study of DTZ on rat skin further demonstrated the efficacy of PVA based film which yielded more than 40.0% cell viability on HaCaT and PBMC cell line with no histological changes on the skin which further confirmed the practical utility of the prepared film.

Topics: Administration, Cutaneous; Alginates; Animals; Biopolymers; Carboxymethylcellulose Sodium; Chitosan; Diltiazem; Drug Delivery Systems; Glucuronic Acid; Heart Failure; Hexuronic Acids; Humans; Hydrophobic and Hydrophilic Interactions; Leukocytes, Mononuclear; Polyvinyl Alcohol; Rats

Topics: Aged, 80 and over; Carboxymethylcellulose Sodium; Drug Eruptions; Drug Hypersensitivity; Drugs, Generic; Excipients; Female; Heart Failure; Humans

The object of this study was to examine whether prolonged-release hard gelatin capsule formulations could be developed for dogs. Different viscosity grades of hydroxypropyl methylcellulose (HPMC) and sodium carboxymethylcellulose (NaCMC) were used to control drug release. Furosemide was chosen because of its wide use in the management of heart failure in dogs. In vitro, selecting different viscosity grades allowed good control of drug release, whereas in vivo the difference between formulations was clearly smaller. Although all formulations gave prolonged release, both inter- and intra-individual variation in the plasma concentration-time curves was high. It is difficult to develop prolonged-release formulations for drugs such as furosemide with highly variable pharmacokinetic properties. However, hard gelatin capsules containing hydrophilic polymers could still be a suitable choice for some drugs.

Topics: Animals; Anticholesteremic Agents; Biological Availability; Capsules; Carboxymethylcellulose Sodium; Chromatography, High Pressure Liquid; Delayed-Action Preparations; Dog Diseases; Dogs; Furosemide; Gelatin; Heart Failure; Hypromellose Derivatives; In Vitro Techniques; Methylcellulose; Viscosity