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 exvivo
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.
Topical spray, Tazarotene Aerosol, Eudragit E100, Thin film.