POSACONAZOLE-LOADED QUATSOMES ENTRAPPED TOPICAL GEL FOR ANTIFUNGAL ACTIVITY: FORMULATION, EX VIVO AND CELL LINE STUDIES
DOI:
https://doi.org/10.22159/ijap.2026v18i4.58029Keywords:
Posaconazole, Quatsomes, Topical gel, Ex-vivo, Activity, MTT assayAbstract
Objective: The present study aimed to formulate and evaluate a posaconazole-loaded quatsomes gel for topical delivery to overcome the poor aqueous solubility of posaconazole and to enhance local drug retention and efficacy.
Methods: Posaconazole-loaded quatsomes were prepared by the thin film hydration method and optimized using a 3² factorial design. The optimized quatsomes were incorporated into a carbopol 940P gel. The formulations were evaluated for pH, viscosity, spreadability, drug content, in vitro drug release, ex vivo skin permeation, activity against Candida albicans, and cytotoxicity using MTT assay on Caco2 and HepG2 cell lines.
Results: Among the developed formulations, F3 showed optimal physicochemical properties with drug content of 96.38±0.42%, suitable viscosity (3201.6 cP), and good spreadability (4.58 g·cm/s). The optimized formulation exhibited sustained drug release 91.6 ± 0.51% at 8 h compared with pure drug gel. The quatsomes gel showed enhanced activity with a zone of inhibition of 23 ± 0.4 mm against Candida albicans. MTT assay demonstrated acceptable cell viability (>80%) at lower concentrations (10 µg/mL), with dose-dependent cytotoxicity at higher concentrations.
Conclusion: Posaconazole-loaded quatsomes gel represents a promising topical delivery system for poorly soluble drugs, offering enhanced efficacy with acceptable safety at therapeutic concentrations.
References
1.Jani RK, Patel ZM, Jani KJ. Formulation and development of posaconazole-loaded controlled release nanosponge topical gel for the treatment of fungal infection. J Pharm Innov. 2025;20:15.doi:10.1007/s12247-024-09912-z.
2.Phatak KM, Yawalkar AN, Sole SS, Vavia PR. Overcoming corneal barriers: posaconazole-loaded cationic surfactant vesicles for enhanced ocular permeability and efficacy. Asian J Pharm Sci. 2025;101087. doi:10.1016/j.ajps.2025.101087.
3.Farooq M, Usman F, Zaib S, Shah HS, Jamil QA, Sheikh FA, et al. Fabrication and evaluation of voriconazole-loaded transethosomal gel for enhanced and anti-leishmanial activity. Molecules. 2022;27(10):3347.doi:10.3390/molecules27103347.
4.Ghurghure SM, Jadhav T, Kale S, Phatak AA. Formulation and evaluation of posaconazole-loaded nanostructured lipid carriers for topical drug delivery system. Curr Trends Pharm Pharm Chem. 2022;4(3):126–134.doi:10.18231/j.ctppc.2022.022.
5.Rukari T, Pingale PL, Upasani CD. Optimizing novasomes: impact of oleic acid and co-surfactant ratio on posaconazole delivery: in vitro and ex vivo pharmacokinetic study. J Appl Pharm Res. 2024;12(3):88–98. doi:10.69857/joapr.v12i3.536.
6.Prathmesh DS, Ruhy Z, Reddy A. Formulation development and characterization of posaconazole-loaded nanoparticle gel. J Pharm Biol Res. 2025;13(2):81–89.
doi:10.30904/j.jpbr.2025.4886.
7.Ali AA, Raja K, Soundarapandi P, Sakthivel S, Venugopal V. Formulation and evaluation of retinoic acid-loaded quatsomes for topical application. J Young Pharm. 2025;17(1):187–193.doi:10.5530/jyp.20251558.
8. Durgun ME, Mesut B, Hacıoğlu M, Güngör S, Özsoy Y. Optimization of micellar-based in situ gelling systems of posaconazole using quality by design approach. Pharmaceutics. 2022;14(3):526. doi:10.3390/pharmaceutics14030526.
9.Lakshmi PK, Marka K, Aishwarya S, Shyamala B. Formulation and evaluation of ibuprofen topical gel: a novel approach for penetration enhancement. Int J Appl Pharm. 2011;3:25–30.
10.Kumar V, Kumar R, Jain VK, Nagpal S. Comparison of virosome versus liposome as drug delivery vehicles using HepG2 and Caco-2 cell lines. J Microencapsul. 2021;38(5):263–275.
doi:10.1080/02652048.2021.1902009.
11. Indira Muzib Y. Posaconazole-loaded quatsomes for topical delivery: development and optimization by 3² factorial design. Vasc Endovascular Rev. 2025;8(Suppl 19):252–263.
12.Bharat P, Atul K, Ajay C. Formulation and evaluation of gel containing miconazole nitrate as an agent. Int J Pharm Res Rev. 2013;2:18–28.
13.Hamza SM, Saleh ZT. Formulation strategy for stable posaconazole nanoemulsion: application of pseudoternary phase diagram. Int J Appl Pharm. 2025;17(5):426–435.
doi:10.22159/ijap.2025v17i5.55055.
14.Albash R, Al-Mahallawi AM, Hassan M, Alaa-Eldin AA. Development and optimization of terpesomes for ocular delivery. Int J Nanomedicine. 2021;16:609–621.doi:10.2147/IJN.S287615.
15.Nazzaro F, Fratianni F, Coppola R, De Feo V. Essential oils and activity. Pharmaceuticals (Basel). 2017;10(4):86. doi:10.3390/ph10040086.
16.Sawwashe D, Chougale RD, Gavande G, Patil KS, Patki S, D’Souza J, et al. Design, development, and characterization of posaconazole ethosomal in situ gel. Thai J Pharm Sci. 2023;47(4):5.
17. Reddy GK, Padmavathi AR, Nancharaiah YV. Fungal infections: pathogenesis, s, and alternate treatment approaches. Curr Res Microb Sci. 2022;3:100137.
doi:10.1016/j.crmicr.2022.100137.
18.Kurane A, Chougale R, Thakur V, Patil K, Patki S, D’Souza J, et al. Development of lyophilized posaconazole-loaded mixed micelles. Fabad J Pharm Sci. 2024;49(1):143–162.
19.Teixeira AD, Quaresma ADV, Branquinho RT, Santos SLEN, Magalhaes JTD, Silva FHRD, et al. Miconazole-loaded nanoparticles coated with hyaluronic acid. Eur J Pharm Sci. 2023;188:106508. doi:10.1016/j.ejps.2023.106508.
20. Iqbal MA, Md S, Sahni JK, Baboota S, Dang S, Ali J. Nanostructured lipid carriers: recent advances. J Drug Target. 2012;20(10):813–830. doi:10.3109/1061186X.2012.716845 .
21.Alvarez L, Kumaran KS, Nitha B, Sivasubramani K. Evaluation of Candida albicans isolates. Braz J Microbiol. 2025;56(1):353–364.doi:10.1007/s42770-024-01558-w.
22.Fernandes Costa A, Evangelista Araujo D, Santos Cabral M, Teles Brito I, Borges de Menezes Leite L, Pereira M. Polymeric nanoparticles for candidiasis. Med Mycol. 2019;57(1):52–62. doi:10.1093/mmy/myx155.
23. Patel D, Dasgupta S, Dey S, Ramani YR, Ray S, Mazumder B. NLC-based gel for topical delivery of aceclofenac. Scientia Pharm. 2012;80(3):749–764. doi:10.3797/scipharm.1202-12.
24. Mahmoud DA, Hassanein NM, Youssef KA, Abouzeid MA. activity of neem extracts. Braz J Microbiol. 2011;42:1007–1016.doi:10.1590/S1517-83822011000300027.
25.Lea T. Caco-2 cell line. In: Verhoeckx K, Cotter P, López-Expósito I, et al., editors. The impact of food bioactives on health. Cham: Springer; 2015. p. 103–111. doi:10.1007/978-3-319-16104-4-10.
26. Balouiri M, Sadiki M, Ibnsouda SK. Methods for in vitro evaluating antimicrobial activity. J Pharm Anal. 2016;6(2):71–9.doi:10.1016/j.jpha.2015.11.005.
27. Mosmann T. Rapid colorimetric assay for cellular growth and survival: application to proliferation and cytotoxicity assays. J Immunol Methods. 1983;65(1-2):55–63.
doi:10.1016/0022-1759(83)90303-4.
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