ABSTRACT
The objective of the study was to develop a suitable trans-dermal delivery system for propranolol hydrochloride (PPL) via employing chitosan as a film former. Drug concentration uniformity, thickness, moisture uptake capacity and skin bioadhesion of the films were characterized. The effects of chitosan and PPL concentration and different penetration enhancers on the release and permeation profiles from the films were investigated. Skin irritation of the candidate film was evaluated. Chitosan film (PPL 2 mg cm(-2), chitosan 2%, m/m, cineol 10%, m/m) was found nonirritant and achieved 88.2% release after 8 hours in phosphate buffer. Significant high (p < 0.001) permeation of PPL through rat skin was obtained using this film compared to the film without enhancer (about 8 times enhancement factor), making it a promising trans-dermal delivery system for PPL.
Subject(s)
Antihypertensive Agents/administration & dosage , Delayed-Action Preparations , Drug Compounding , Drug Delivery Systems , Propranolol/administration & dosage , Adhesives/chemistry , Adhesives/metabolism , Administration, Cutaneous , Animals , Antihypertensive Agents/chemistry , Antihypertensive Agents/pharmacokinetics , Antihypertensive Agents/pharmacology , Benzalkonium Compounds/chemistry , Chitosan/chemistry , Drug Evaluation, Preclinical , Excipients/chemistry , Male , Oleic Acid/chemistry , Permeability , Polysorbates/chemistry , Propranolol/chemistry , Propranolol/pharmacokinetics , Propranolol/pharmacology , Rats , Rats, Wistar , Skin/metabolism , Skin Absorption , Surface-Active Agents/analysis , Surface-Active Agents/chemistry , Terpenes/chemistry , Time FactorsABSTRACT
The aim of the study was to develop a Meloxicam (ME) transdermal gel formulations based on complexation with ß-cyclodextrin. ME ß-Cyclodextrin gel formulations were prepared using four different gel bases with different concentrations and different permeation enhancers. The developed formulations were examined for their in vitro characteristics and their diffusion through a mouse skin. The gel formulations were prepared successfully. Physicochemical characterization of ME ß-CD complex in solution state by phase solubility revealed 1:1 M complexation of ME with ß-Cyclodextrin. ME release profiles from the inclusion complex were superior over ME alone. Hydroxypropyl methyl cellulose 15% w/w gel base was proven to be a suitable base for ME inclusion complex formulation as it provides a high drug release than other studied bases. ME ß-CD complex gel formulations containing oleic acid (1% w/w) or (5% w/w) cineol used as permeation enhancers in (15% w/w) HPMC gel base were proven to provide a higher diffusion rate of the drug through the mouse skin. This is very promising in providing analgesic activity of meloxicam via topical route of administration.
