Objective: The objective of the present study was to formulate a novel topical spray containing Antiacne agent. Comprising drug and other non-toxic excipients (mixture of propane and butane) LPG as propellant. Study was designed to increase the absorption of drug from the human skin. Therefore clear clinical need exists for development of suitable formulation of drug that has improved permeability and absorption, with the potential transparent thin film with the once daily dosing. An optimum formulation was to be study for skin irritation study, in-vivo drug release and finally for stability study.
Experimental work: The preformulation studies for drug was carried out and compatibility of drug in formulation with different excipients was checked. Solutions for topical sprays were filled in Aluminium containers fitted with continuous spray valve. Primary screening of variables like polymers, penetration enhancers and solvents were done by preparing trial batches. Final batches were prepared comprising of polymer Eudragit E100 (flim forming
polymer), penetration enhancers such as IPM and PG act as plasticizer, solvent and co-solvent such as Iso Propyl alcohol and ethanol respectively. Prepared Tazarotene topical spray formulations were evaluated for different parameters. Tazarotene topical spray included determination of delivery rate, delivery amount, pressure test, drug content, minimum fill, leakage test, flammability, spray patterns, particles size, etc and as well as In-vivo Skin irritation study and In-vitro drug released, Finally, optimised formulation Was kept for stability study as per ICH guidelines.
Results and discussion: Absence of physical and chemical incompatibility during compatibility study revealed that Tazarotene is compatible with container closure and excipients. Tazarotene topical spray formulation T6 was found to be the best formulation Evaluation data of different formulation for Physico-chemical test, performance test and ex- vivo diffusion studies indicated the effectiveness of IPM as penetration enhancer. T6 was further proved non irritant and stability study in accordance with ICH guidelines indicated that the optimised formulation was stable.
Conclusions: A novel type of formulation comprised of Tazarotene, Eudragit E100, IPM and organic volatile and non-volatile solvents, was used to develop a new topical spray
formulation. This novel topical spray formulation was transparent solution with good, early evaporation and ease of application. In addition the research results showed the resultant invisible thin film with excellent carrier and permeability enhanced effect of IPM on drug. Finally, skin irritation test proved that the spray formulation was safe to be used for topical delivery. In summary, the novel formulation of Tazarotene, Eudragit E100, IPM and other excipients may provide alternate dosage form to Tazarotene gel formulation.
Key-words:. Topical spray, Tazarotene Aerosol, Eudragit E100, Thin film.