EUDRAGIT S-100 MICROSPONGES BASED GEL OF BUTENAFINE HYDROCHLORIDE FOR CANDIDIASIS: DESIGN, OPTIMIZATION, IN VITRO AND IN VIVO INVESTIGATION

SHAILESH  WADHER; ASHWINI  POTULWAR; SANJAY  PEKAMWAR; SHRADHA  TIWARI

doi:10.22159/ajpcr.2025v18i4.54174

Authors

SHAILESH WADHER Department of Quality Assurance, School of Pharmacy, Swami Ramanand Teerth Marathwada University, Nanded-431606
ASHWINI POTULWAR Department of Pharmaceutics School of Pharmacy, Swami Ramanand Teerth Marathwada University, Nanded-431606 and Poona College of Pharmacy, Bharati Vidyapeeth (Deemed To Be University), Erandwane, Pune-411038 https://orcid.org/0009-0009-9223-7542
SANJAY PEKAMWAR Department of Pharmaceutical Chemistry, School of Pharmacy, Swami Ramanand Teerth Marathwada University, Nanded-431606 https://orcid.org/0000-0003-4308-071X
SHRADHA TIWARI Department of Pharmaceutics, School of Pharmacy, MIT Vishwaprayag University, Solapur Pune Highway, Kegaon, Solapur, 413255 https://orcid.org/0000-0001-7608-6240

DOI:

https://doi.org/10.22159/ajpcr.2025v18i4.54174

Keywords:

Butenafine hydrochloride, Microsponge, Quasi-emulsion solvent diffusion, Topical gel, Microsponge loaded gel

Abstract

Objective:This research focused on formulating a controlled-release microsponge gel incorporating Butenafine hydrochloride (BFH), designed to enhance drug retention time and reduce the risk of skin irritation.

Methods:BFH-loaded microsponges were prepared using the quasi-emulsion solvent diffusion technique. Optimization of formulation parameters, including eudragit S-100 and dichloromethane, was performed using a 3²-factorial design. The microsponges were evaluated for production yield, entrapment efficiency, and cumulative drug release using FTIR, XRD, DSC, and SEM techniques. The optimized microsponge formulation was incorporated into a Carbopol 934 gel. The resulting microsponge gel was assessed for extrudability, spreadability, drug content, in-vitro drug release, rheological properties, and in-vitro antifungal activity against Candida albicans.

Results:The optimized microsponge formulation exhibited a particle size of 48.92 ± 2.49 µm, an entrapment efficiency of 89.42 ± 1.55%, and a cumulative drug release of 81.67 ± 2.41%. The microsponge gel demonstrated a controlled drug release and was non-irritant to rat skin. The controlled release of butenafine hydrochloride from the microsponge gel resulted in prolonged drug retention with reduced permeation activity.

Conclusion:The study revealed that the butenafine hydrochloride microsponge gel offers enhanced topical retention and prolonged drug release. Additionally, it showed superior antifungal activity compared to marketed preparations while significantly reducing skin irritation.

Downloads

Download data is not yet available.

References

Borawake PD, Arumugam K, Shinde JV, Chavan RS. Microsponge as an emerging technique in novel drug delivery system. J Drug Deliv Ther. 2021;11(1):171-82. doi: 10.22270/jddt.v11i1.4492

Balijepalli MK, Chandra SP, Taraka R. Formulation and optimization of floating sustaind release tablets of atazanavir sulfate through box-behnken design. Asian J Pharm Clin Res. 2025;18:75-86. doi: 10.22159/ ajpcr.2025v18i3.53791

Hong J, Chen H, Xiang S, Zuo T, Cao S, Liu L, et al. Toward application of microsponges in transdermal drug delivery system. MOJ Bioequiv. 2015;1(1):7-12. doi: 10.15406/mojbb.2015.01.00003

Amrutiya N, Bajaj A, Madan M. Development of microsponges for topical delivery of mupirocin. AAPS Pharm Sci Tech. 2009;10(2):402-9. doi: 10.1208/s12249-009-9220-7

Yadav KS, Kale K. High pressure homogenizer in pharmaceuticals: Understanding its critical processing parameters and application. J Pharm Innov. 2019;15:1-12. doi: 10.1007/s12247-019-09413-4

Oza NA, Sahoo S, Oza S. A 32 full factorial design for topical controlled releasetazarotene microsponge using HPMC gel. Int J Appl Pharm. 2019;11:12-8. doi: 10.22159/ijap.2019v11i5.34496

Pawar A, Gholap AP, Kuchekar AB, Bothiraja C, Mali AJ. Formulation and evaluation of optimized oxybenzone microsponge gel for topical delivery. J Drug Deliv. 2015;2015:261068. doi: 10.1155/2015/261068

Mohan D, Gupta VR. Microsponge based drug delivery system of voriconazole for fungal infection: Formulation development and in-vitro evaluation. J Drug Deliv Ther. 2019;9(3):369-78. doi: 10.22270/jddt. v9i3.2840

Yadav V, Jadhav P, Dombe S, Bodhe A, Salunkhe P. Formulation and evaluation of microsponge gel for topical delivery of antifungal drug. Int J Appl Pharm. 2017;9:30-7. doi: 10.22159/ijap.2017v9i4.17760

Khurshid MF, Hussain T, Masood R, Hussain N. Development and evaluation of a controlled drug delivery wound dressing based on polymeric porous microspheres. J Ind Text. 2015;46:986-99. doi: 10.1177/1528083715612231

Chellam B, Gholap AD, Shaikh K, Pawar P. Investigation of ethyl cellulose microsponge gel for topical delivery of eberconazole nitrate for fungal therapy. Ther Deliv. 2014;5(7):781-94. doi: 10.4155/tde.14.43

Kumar PM, Ghosh A. Development and evaluation of silver sulfadiazine-loaded microsponge-based gel for partial thickness (second-degree) burn wounds. Eur J Pharm Sci. 2017;96:243-54. doi: 10.1016/j.ejps.2016.09.038

Bhatia M, Saini M. Formulation and evaluation of curcumin microsponges for oral and topical drug delivery. Prog Biomater. 2018;7:239-48. doi: 10.1007/s40204-018-0099-9

Patel UB, Shah C. Formulation and development of aceclofenac loaded microsponges topical drug delivery system using quality by design approach. Int J Adv Pharm. 2018;7(4):17-32. doi: 10.52711/0975- 4377.2021.00033

Pandey P, Mishra SK, Kapoor A, Sharma N, Kumari P. Tolnaftate microsponges embedded biocompatible gels for controlled and effective antidermatophytic activity. Int Res J Pharm. 2018;9(6):128-33. doi: 10.7897/2230-8407.096103

Kinjal P, Mahesh N, Pankit D, Jigar V, Umeash U. Formulation and evaluation of ciclopirox olamine microsponge based topical gel. Invent Rapid NDDS. 2014;2014(3):1-5.

Enkelej G, Entela H, Skerdil X, Ledjan M. Formulation and in vitro evaluation of diclofenac sodium gel. Int J Pharm Pharm Sci. 2014;6(4):564-6.

Rizkalla CM, Aziz RL, Soliman II. In vitro and in vivo evaluation of hydroxyzine hydrochloride microsponges for topical delivery. AAPS Pharm Sci Tech. 2011;12(3):989-1001. doi: 10.1208/s12249-011-9663-5

Patel P, Monpara M, Mandal S, Patel N. Formulation and evaluation of microemulsion based gel of itraconazole. Pharmagene. 2013;1(2):32-6.

Sun L, Zhou S, Wang W, Li X, Wang J, Weng J. Preparation and characterization of porous biodegradable microspheres used for controlled protein delivery. Colloids Surf A Physicochem Asp. 2009;345:173-81. doi: 10.1016/j.colsurfa.2009.05.016

Jelvehgari M, Siahi-Sadbad MR, Azarmi S, Martin GP, Nokhodchi A. The microsponge delivery system of benzoyl peroxide: Preparation, characterization and release studies. Int J Pharm. 2006;308:124-32. doi: 10.1016/j.ijpharm.2005.11.001

Salah S, Awad GE, Makhlouf AI. Improved vaginal retention and enhanced antifungal activity of miconazole microsponges gel: Formulation development and in vivo therapeutic efficacy in rats. Eur J Pharm Sci. 2018;114:255-66. doi: 10.1016/j.ejps.2017.12.023

Mahapatra AP, Patil V, Patil RY. Solubility enhancement of poorly soluble drugs by using novel techniques: A comprehensive review. Int J Pharm Tech Res. 2020;13(2):80-93.

Kamaly N, Yameen B, Wu J, Farokhzad OC. Degradable controlled-release polymers and polymeric nanoparticles: Mechanisms of controlling drug release. Chem Rev. 2016;116(4):2602-63. doi: 10.1021/ acs.chemrev.5b00346

Alexander IB, Krasnyuk II, Natalia BD, Michael SZ, Maria NA, Elena OB. Dermatologic gels spreadability measuring methods comparative study. Int J Appl Pharm. 2022;14(1):164-8. doi: 10.22159/ ijap.2022v14i1.41267

Kalaydina RV, Bajwa K, Qorri B, Decarlo A, Szewczuk MR. Recent advances in “smart” delivery systems for extended drug release in cancer therapy. Int J Nanomedicine. 2018;13:4727-45. doi: 10.2147/IJN.S167707

Patil ST, Patil HI, Vanjari AV, Wadkar KA. Formulation of tolnaftate loaded cubosomes for effective transdermal delivery: An in vitro and ex vivo study. Int J Curr Pharm Res. 2025;17(1):33-2. doi: 10.22159/ ijcpr.2025v17i1.6016