Please use this identifier to cite or link to this item: http://scholarbank.nus.edu.sg/handle/10635/16464
Title: Liposomal preparations of benzoyl peroxide for the treatment of acne
Authors: ONG SHWU YNG
Keywords: Nano-liposomes; Acne Treatment; Benzoyl Peroxide; Topical Drug Delivery; Propionibacterium acnes; Antibacterial Activity
Issue Date: 21-Sep-2005
Source: ONG SHWU YNG (2005-09-21). Liposomal preparations of benzoyl peroxide for the treatment of acne. ScholarBank@NUS Repository.
Abstract: Benzoyl Peroxide (BPO), used for treating acne, is known to cause concentration-dependent skin irritation. This may be prevented by developing a delivery system in which BPO is encapsulated in liposomes. The objectives of this study were to develop, optimize and characterize liposomal preparations of BPO, and to determine its antibacterial efficacy and storage stability. Phosphatidylcholine (PC) and cholesterol (CH) in the mole ratio of 3:1 were used to prepare nano-sized BPO liposomes with BPO content of 0.377 mg/ml and high drug encapsulation efficiency of >90%. The pressure applied during solvent evaporation was important, with low pressure resulting in substantial drug loss. The liposomes exhibited a sustained release of the encapsulated BPO, with less than 40% of the drug load released in 24h. A longer duration of sonication produced smaller particles with a greater propensity to form aggregates, leading to slower rate of drug release.Increasing the BPO loading concentration to 12.5 to 100 mg/ml resulted in lower drug encapsulation efficiency of 71 to 78%. However, the in vitro drug release profiles were comparable to those for liposomes with low BPO loadings. The properties of the BPO-loaded liposomes were not significantly changed by increasing the cholesterol content in the lipid bilayers to PC: CH ratio of 1:1. Liposomes prepared with PC: CH ratios of 3:1 and 1:1, and with loading BPO concentration of 25 mg/ml or higher were effective in preventing the proliferation of P. acnes.Liposomes prepared with PC:CH ratio of 3:1 were unstable upon storage. This is evidenced by their erratic change in size, with liposomes stored in the fridge increasing in size to more than 2000nm and those stored under room temperature decreasing in size to between 200 and 400 nm. Liposomes prepared with PC:CH ratio of 1:1 were more stable in that they exhibited much smaller changes in particle size upon storage. Storage also caused the leakage of BPO from the liposomes prepared with PC:CH ratio of 1:1, the encapsulation efficiency reducing to 60 - 65% after 3 weeks storage at either room temperature or in the fridge. In addition, storage enhanced the antibacterial efficacy of the BPO-loaded liposomes prepared with PC:CH ratio of 3:1 and 1:1. From these results, it is clear that BPO can be stably encapsulated in liposomes prepared with PC: CH ratio of 1:1 without losing its antibacterial effect against P. acnes.
URI: http://scholarbank.nus.edu.sg/handle/10635/16464
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