PROCESS VALIDATION OF BETA-SITOSTEROL HAIR GEL FORMULATION AND EVALUATION OF 5 ALPHA REDUCTASE INHIBITION IN VITRO FOR THE TREATMENT OF ANDROGENETIC ALOPECIA

Authors

  • ARPAN CHAKRABORTY Department of Pharmaceutical Sciences and Technology, MAKAUT University, Haringhata, West Bengal, India https://orcid.org/0000-0001-5123-0672
  • ARKA BHATTACHARJEE Department of Pharmaceutical Sciences and Technology, MAKAUT University, Haringhata, West Bengal, India https://orcid.org/0000-0003-0376-6987
  • MANAS CHAKRABORTY Calcutta Institute of Pharmaceutical Technology & Allied Health Sciences, Uluberia, Howrah, West Bengal, India https://orcid.org/0000-0001-7521-0617
  • GOUTAM MUKHOPADHYAY BCDA College of Pharmacy and Technology, Hridaypur, Barasat, 24pgs. (North), West Bengal, India

DOI:

https://doi.org/10.22159/ijap.2023v15i2.46757

Keywords:

5α-reductase, hair loss, beta-sitosterol, NADPH, HPTLC, hair gel, alopecia

Abstract

Objective: The present study was aimed to develop topical gel containing β-sitosterol using carbopol 940 as gelling agent and to investigate 5 alpha reductase (5α-reductase) inhibitory activity of suitable gel formulation and compare it with a commercial product used topically for alopecia.

Methods: Three different batches of β-sitosterol hair gel formulation were manufactured and evaluated. Additionally, the 5α-reductase inhibitory activity of the prepared formulation, finasteride as a positive control, was evaluated and compared to the commercial herbal formulation used.

Results: According to the analytical findings of three different batches, the gel formulation is good in appearance, homogeneous, and easily spreadable. Based on findings from HPLC and HPTLC, the amount of β-sitosterol in those formulations complies with the label claim. By checking different critical parameters of those batches, we established the manufacturing process method validation and the process reproducibility. In-vitro results showed the good 5α-reductase inhibitory potential of prepared gel formulation and then commercial product. The IC50 value of the prepared formulation was 118.960 ± 0.634 (µg/ml) and standard beta-sitosterol 88.854 ± 0.70 (µg/ml), whereas Finasteride (positive control) 224.372 ± 3.103 (ng/ml).

Conclusion: Thus, β-sitosterol formulation utilises a straightforward, low-cost production, less time-consuming process with minimal facility and equipment requirements. The formulation may be a promising candidate for future investigation into their antiandrogenic activities.

Downloads

Download data is not yet available.

References

Sperling LC. Hair and systemic disease. Dermatol Clin. 2001;19(4):711–726. doi: 10.1016/S0733-8635(05)70310-7

Kumar N, Chaiyasut C. Hair growth promoting activity of Carthamus tinctorius florets extract-loaded nanostructured lipid carriers. Int J Pharm Pharm Sci. 2015;7(2):252-7.

Levy MA, Brandt M, Sheedy KM, Holt DA, Heaslip JI, Trill JJ, Ryan PJ, Morris R, Garrison LM, Bergsma DJ. Cloning, expression and functional characterization of type 1 and type 2 steroid 5α-reductase from Cynomolgus monkey: comparisons with human and rat isoenzymes. J Steroid Biochem Mol Biol. 1995;52(4):307-19. doi: 10.1016/0960-0760(94)00183-M

Nutbrown M, Hull SP, Cunliffe WJ, Randall VA. Abnormalities in the ultrastructure of melanocytes and the outer root sheath of clinically normal hair follicles from alopecia areata scalps. J Invest Dermatol. 1995;104(5):12S–13S. doi: 10.1038/jid.1995.34

Guarna A, Poletti A, Catrambone F, Danza G, Marrucci A, Serio M, Celotti F, Martini, L. Synthesis of a chemiluminescent probe useful for the purification of steroid 5α-reductase. Bioorg Med Chem Lett. 1996;6(16),1997-2002.doi: 10.1016/0960-894X(96)00360-5

Erum SA, Sultan SA, Shah SA, Ashraf MU, Choudhary MI. Microbial Oxidation of Finasteride With Macrophomina Phaseolina (Kucc 730). Int J Pharm Pharm Sci. 2017;9(11):17-20. doi: 10.22159/ijpps.2017v9i11.13576

DoSH,AhnRS,NaMS,JuHR. Improvement of alopecia and decreases in hair cortisol and dihydrotestosterone concentrations after the topical use of plant extracts in men with androgenetic alopecia. Asian J Pharm Clin Res. 2021;14(8),71-9. doi: doi.org/10.22159/ajpcr.2021.v14i8.41859

Salle ED, Giudici D, Radice A, Zaccheo T, Ornati G, Nesi M, Panzeri A, Delos S, Martin PM. PNU 157706, a novel dual type I and II5α-reductase inhibitor. J Steroid Biochem Mol Biol. 1998;64(3-4):179-86.doi:10.1016/S0960-0760(97)00158-1

Jadhav VM, Thorat RM, Kadam VJ, Gholve SB. Kesharaja: hair vitalizing herbs. Int J Pharmtech Res.2009;1(3):454-67.

Prager N, Bickett K, French N, Marcovici G. A randomized, double-blind, placebo-controlled trial to determine the effectiveness of botanically derived inhibitors of 5α-reductase in the treatment of androgenetic alopecia. J Altern Complement Med. 2002;8(2):143-52. doi: 10.1089/acm.2002.8.143

https://www.adamonline.com/en/product/1022138-riaheal-ointment-15g

Jewo PI, Fadeyibi IO, Babalola OS, Saalu LC, Benebo AS, Izegbu MC, Ashiru OA. A.comparative study of the wound healing properties of moist exposed burn ointment (MEBO) and silver sulphadiazine. Ann. Burns Fire Disasters. 2009;22(2):79-82. PMID: 21991159

Moreau RA, Whitaker BD, Hicks KB.Phytosterols, phytostanols, and their conjugates in foods: structural diversity, quantitative analysis, and health-promoting uses. Prog Lipid Res. 2002;41(6):457-500. doi: 10.1016/s0163-7827(02)00006-1

Zhang F, Liu Z, He X, Li Z, Shi B, Cai B.β-sitosterol-loaded solid lipid nanoparticles ameliorate complete freund’s adjuvant-induced arthritis in rats: involvement of NF-КB and HO-1/Nrf-2 pathway. Drug Deliv. 2020;27(1):1329-1341. doi: 10.1080/10717544.2020.1818883

Upadhyay K, Gupta NK, Dixit VK. Development and characterization of phyto-vesicles of β-sitosterol for the treatment of androgenetic alopecia. Arch Dermatol Res. 2012;304:511-9. doi: 10.1007/s00403-011-1199-8

Prabahar K, Udhumansha U, Elsherbiny N, Qushawy M. Microneedle mediated transdermal delivery of β-sitosterol loaded nanostructured lipid nanoparticles for androgenic alopecia. Drug Delivery. 2022;29(1): 3022-3034. doi: 10.1080/10717544.2022.2120927

Bariya SH, Gohel MC, Mehta TA, Sharma OP. Microneedles: an emerging transdermal drug delivery system. J Phar & Pharmaco. 2012;64(1):11-29. doi: 10.1111/j.2042-7158.2011.01369.x

Mishra US, Murthy PN, Pasa G, Kumar S. Formulation development and standardisation of herbal gel containing methanolic extract of Butea frondosa. Int Res J Pharm. 2011;2:126-9.

Gupta V.Formulation and evaluation of naproxen gel containing tulsi oil as penetration enhancer. Int J Pharm Clinical Res.2009;1(3):153-5.

Verma A, Singh S, Kaur R, Jain UK. Formulation and evaluation of clobetasol propionate gel. Asian J Pharm Clin Res. 2013;6:15-8.

Ramakrishna S, Gopikrishna UV. Formulation and Evaluation of Herbal Hair Gel. Sch Int J Tradit Complement Med.2022;5(2):28-32.

Jyothi D, Koland M. Formulation and evaluation of an herbal anti-inflammatory gel containing Trigonella foenum greacum seed extract. Int J Pharm Pharm Sci. 2016;8(1):41-4.

Bhattacharjee A, Chakraborty A, Dutta D, Mukhopadhyay G. Standardization of Eclipta Alba by HPTLC, HPLC and AAS. Pharm Anal Acta. 2017;8(3):1-6.

Nahata A, Dixit VK. Evaluation of 5α‐reductase inhibitory activity of certain herbs useful as antiandrogens. Andrologia. 2014;46(6):592-601. doi: 10.1111/and.12115

Ping S, Xingquan Z. Relationship between the elemental content and pH of human hair. Sci Total Environ. 1993;128(2-3):151-6. doi: 10.1016/0048-9697(93)90217-T

Cabeza M, Bratoef E, Heuze I, Ramírez E, Sánchez M,Flores E.Effect of beta-sitosterol as inhibitor of 5alpha-reductase in hamster prostate. Proc West Pharmacol Soc. 2003;2003;46:153-5. PMID: 14699915

Zamani P, Mokhtari O, Dehghanian F. Identification of Beta-Sitosterol and Stigmasterol as Possible Inhibitors of 5 Alpha-Reductase 1: An In-Silico Study. Precis Med Clin OMICS.2022;1(1):1-8. doi: 10.5812/pmco.121545

Roy RK, Thakur M,Dixit VK. Hair growth promoting activity of Eclipta alba in male albino rats. Arch Dermatol.2008;300(7):357-64. doi: 10.1007/s00403-008-0860-3

Prager N, Bickett K, French N, Marcovici G.A randomized, double-blind, placebo-controlled trial to determine the eVectiveness of botanically derived inhibitors of 5α-reductase in the treatment of androgenetic alopecia. J Alt Compl Med.2002;8(2):143–52. doi: 10.1089/acm.2002.8.143

Published

29-12-2022

How to Cite

CHAKRABORTY, A., BHATTACHARJEE, A., CHAKRABORTY, M., & MUKHOPADHYAY, G. (2022). PROCESS VALIDATION OF BETA-SITOSTEROL HAIR GEL FORMULATION AND EVALUATION OF 5 ALPHA REDUCTASE INHIBITION IN VITRO FOR THE TREATMENT OF ANDROGENETIC ALOPECIA. International Journal of Applied Pharmaceutics, 15(2). https://doi.org/10.22159/ijap.2023v15i2.46757

Issue

Section

Original Article(s)