Alopecia is a psychologically distressing phenomenon. Androgenetic alopecia (AGA) is the most common form of alopecia, which affects millions of men and women worldwide, and is an androgen driven disorder. To study the effect of β-sitosterol phyto-vesicles on AGA, the testosterone-induced alopecia model was used. For the study, the albino rats were used and the period of study was 21 days. β-Sitosterol is a phytosterol which is chemically similar to cholesterol. This compound was found suitable for the preparation of phyto-vesicles by the process involving its complexation with phosphatidyl choline. Pharmacokinetic studies of β-sitosterol reveal its poor absorption through the intestine. The objective of the present study is to enhance the bioavailability of β-sitosterol by its complexation with phosphatidyl choline and then to formulate it as phyto-vesicles for the treatment of alopecia. The complex of β-sitosterol was prepared with phosphatidyl choline and characterized on the basis of solubility, melting point, TLC, UV, IR and NMR spectroscopy. This complex was then formulated as phyto-vesicles and then characterized. The results revealed that effect on alopecia is better in case of phyto-vesicles as compared to the complex, physical mixture and the β-sitosterol itself. Enhanced bioavailability of the β-sitosterol complex may be due to the amphiphilic nature of the complex, which greatly enhance the water and lipid solubility of the compound. The present study clearly indicates the superiority of phyto-vesicles over the complex and β-sitosterol, in terms of better absorption and improved activity for the treatment of alopecia.
The authors would like to acknowledge Acros Organics, New Jersey, USA for the gift sample of β-sitosterol. The authors would also like to thank LIPOID GmbH (Germany) for providing the gift samples of phosphatidyl choline and UGC for providing the financial assistance.
Conflict of interest
The authors declare that they have no conflict of interest.
Gupta NK, Dixit VK (2010) Bioavailability enhancement of curcumin by complexation with phosphatidyl choline. J Pharm Sci 100:1987–1995PubMedCrossRefGoogle Scholar
Gupta NK, Dixit VK (2011) Absorption enhancement of grape seed polyphenols by complexation with phosphatidyl choline. Drug Deliv 18:312–319Google Scholar
Gupta NK, Dixit VK (2011) Development and evaluation of vesicular system for curcumin delivery. Arch Dermatol Res 303(2):89–101PubMedCrossRefGoogle Scholar
Headington JT, Novak E (1984) Clinical and histological studies of male pattern baldness treated with topical minoxidil. Curr Ther Res Clin Exp 36:1098–1106Google Scholar
Mascarella S, Giusti A, Marra F et al (1993) Therapeutic and antilipoperoxidant effects of silybin phosphatidyl choline complex in chronic liver disease: preliminary results. Curr Ther Res 53:98–102CrossRefGoogle Scholar
Matsuoka K, Nakazawa T, Nakamura A, Honda C, Endo K, Tsukada M (2008) Study of thermodynamic parameters for solubilization of plant sterol and stanol in bile salt micelles. Chem Phys Lipids 154:87–93PubMedCrossRefGoogle Scholar
Moreau RA, Whitaker BD, Hicks KB (2002) Phytosterols, phytostanols, and their conjugates in foods: structural diversity, quantitative analysis, and health-promoting uses. Prog Lipid Res 41:457–500PubMedCrossRefGoogle Scholar
Normen AL, Brants HA, Voorrips LE, Andersson HA, Vandenbrandt PA, Goldbohm RA (2001) Plant sterol intakes and colorectal cancer risk in the Netherlands Cohort Study on Diet and Cancer. Am J Clin Nutr 74:141–148PubMedGoogle Scholar
Nutbrown M, Hull SP, Cunliffe WJ, Randall VA (1995) Abnormalities in the ultrastructure of melanocytes and the outer root sheath of clinically normal hair follicles from alopecia areata scalps. J Invest Dermatol 104:12S–13SPubMedCrossRefGoogle Scholar
Prager N, Bickett K, French N, Marcovici G (2002) A randomized, double-blind, placebo-controlled trial to determine the effectiveness of botanically derived inhibitors of 5-α-reductase in the treatment of androgenetic alopecia. J Altern Complement Med 8:143–152PubMedCrossRefGoogle Scholar
Roy RK, Thakur M, Dixit VK (2008) Hair growth promoting activity of Eclipta alba in male albino rats. Arch Dermatol Res 300:357–364PubMedCrossRefGoogle Scholar
Sharma A, Gupta NK, Dixit VK (2010) Complexation with phosphatidyl choline as a strategy for absorption enhancement of boswellic acid. Drug Deliv 17:587–595PubMedCrossRefGoogle Scholar
Swell L, Boiter TA, Field H, Treadwell CR (1956) The absorption of plant sterols and their effect on serum and liver sterol levels. J Nutr 58:385–398PubMedGoogle Scholar
Wilt TJ, MacDonald R, Ishani A (1999) Beta-sitosterol for the treatment of benign prostatic hyperplasia: a systematic review. BJU Int 83:976–983PubMedCrossRefGoogle Scholar
Ying L, Yang DJ, Chen SL et al (2008) Comparative physiochemical characterization of phospholipids complex of puerarin formulated by conventional and supercritical methods. Pharm Res 25:563–577CrossRefGoogle Scholar