Development of topical thymoquinone loaded polymer–lipid hybrid vesicular gel: in-vitro and ex-vivo evaluation

Abstract

Thymoquinone (TH), a naturally occurring moiety shows excellent anticancer properties and in the present study, TH loaded polymer hybrid lipid vesicles (TH PLH) were formulated, and in-vitro cytotoxicity towards breast cancer cell lines (MCF-7 and MBD–MB 231 cells) was determined. TH PLH was primed by the ethanol spraying method and were characterized for various attributes like particle size, morphology, percentage drug entrapment, elasticity, rheological, zeta potential, etc. The prepared TH PLH Vesicles showed an average particle size from 344.7 ± 3.7 nm to 351.9 ± 2.3 nm and showed very narrow distribution with polydispersity index ranging from 0.245 ± 0.36 to 0.271 ± 0.66. The surface charge on the vesicles was confirmed by zeta potential (þ −21.3 ± 1.08 mV to þ −19.98 ± 3.4 mV). The globular moulded vesicles were in the nano-size range and had high flexibility and an approximately 10-fold increase in elasticity properties. TH PLH Vesicular gel was formulated by means of Carbopol 934 and was evaluated for physical appearance, pH, rheological behaviour, and skin irritation test. Cytotoxicity study reveals paramount inhibition on cells by TH vesicle-loaded gel. These results showed the high potential of TH PLH vesicles for topical anticancer application.