Anticancer efficacy of perillyl alcohol-bearing PLGA microparticles

Mohammad Farazuddin¹, Bhawna Sharma², Aijaz Ahmed Khan³, Beenu Joshi², Mohammad Owais^1
1Interdisciplinary Biotechnology Unit, Aligarh Muslim University, Aligarh, Uttar Pradesh, India; ²Immunology Division, NJIL and other Mycobacterial diseases, Agra-282001, Uttar Pradesh, India; ³Department of Anatomy, JN Medical college, Aligarh Muslim University, Aligarh-202002, Uttar Pradesh, India

Abstract: In the present study, a novel poly-lactic glycolic acid (PLGA)-based microparticle formulation of perillyl alcohol (POH) was prepared and characterized. Further, its efficacy was evaluated against di-methyl benzo anthracene-induced skin papilloma in Swiss albino mice. The characterization studies showed that POH-bearing PLGA microparticles were of the size 768 ± 215 nm with a ζ-potential value of -7.56 ± 0.88 mV. The entrapment efficiency of the active drug in particles was 42.4% ± 3.5%. POH-bearing PLGA microparticles were stable and released entrapped drug gradually over an extended time period. The in vitro efficacy of POH-bearing PLGA microparticles was evaluated by examining their differential cytotoxicity and assessing their ability to inhibit epidermoid carcinoma cell line (A253). The POH-based microparticles when administered to tumor-bearing animals caused greater tumor regression and increased survival rate (~80%) as compared with the group receiving free form of POH (survival rate 40%). The superiority of POH-PLGA microparticles over free form of POH was further evident from their ability to modulate apoptosis-regulating factors.

Keywords: poly-lactic glycolic acid, epidermoid cancer cells, skin papilloma, anticancer efficacy