DESIGN, FORMULATION, AND CHARACTERIZATION OF LIPOSOMAL-ENCAPSULATED GEL FOR TRANSDERMAL DELIVERY OF FLUCONAZOLE
Objectives: The present objective for the study was to prepare proliposomal gel bearing an antifungal agent, fluconazole (FLZ) intended for topical application.
Methods: Various proliposome formulations were prepared using thin-film hydration technique by varying the lipid phase composition (phosphatidylcholine/cholesterol). Proliposome formulations were characterized for vesicle size, vesicle size distribution, vesicle morphology, drug content, entrapment efficiency, percentage yield value, storage stability analysis, Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), in vitro diffusion study, release kinetic studies, and antifungal activity. Topical proliposomal gels were prepared by incorporation of lyophilized proliposome into a structured vehicle carbopol 934 (2.5%).
Results: A spherical shape of reconstituted FLZ liposome with an average vesicle about 5â€“8 Î¼m was observed in photomicrographs. The percentage entrapment of drug was increased with increase in phospholipid composition in the range of 55.13â€“69.61%. The FTIR and DSC studies showed no possible drug-excipient interaction. Proliposomal gel showed the prolonged release of FLZ than the lyophilized liposomes. The release kinetic values of regression coefficients confirmed the diffusion-dependent release of the drug. Stability studies indicated that product is stable and should be stored at low temperature.
Conclusion: The proposed FLZ proliposomal gel showed sustained release with enhanced antifungal activity implicating its potential in effective transdermal delivery for the topical pharmacotherapy.
2. Agnieszka EW, Emilian A. Interfacial properties of phosphatidylcholine-based dispersed systems. Ind Eng Chem Res 2015;54:6489-96.
3. Zhenjun H, Xuan L, Ting Z, Yanzhi S, Zhennan S, Jing L, et al. Progress involving new techniques for liposome preparation. Asian J Pharm Sci 2014;9:176-82.
4. Maximiliano G, Claudia S, Carlos B, Adriana MC. Percutaneous drug delivery systems for improving antifungal therapy effectiveness: A review. Int J Pharm Pharm Sci 2014;6:8-16.
5. Loveleenpreet K, Prabhjot K, Khan MU. Liposome as a drug carrier-A review. Int J Res Pharm Chem 2013;3:121-8.
6. Kamra M, Diwan A. Liposomes in dermatological diseases. J Appl Pharm Res 2017;5:1-8.
7. Bhupendra P, Narendra K, Suman S, Amit R. Liposome: Method of preparation, advantages, evaluation and its application. J Appl Pharm Res 2015;3:1-8.
8. Gyati S, Davinder S, Abhay A. Novel vesicular carriers for topical drug delivery and their applications. Int J Pharm Sci Rev Res 2013;21:77-86.
9. Marilene E, Maria HA, Jaime C, JosÃ© MS. Evolution of liposomal carriers intended to anticancer drug delivery: An overview. Int J Curr Pharm Res 2015;7:26-33.
10. Prasanthi D, Lakshmi PK. Vesicles-mechanism of transdermal permeation: A Review. Asian J Pharm Clin Res 2012;5:18-25.
11. Sudipta D, Arnab S, Ananya B. Design, development and evaluation of fluconazole topical gel. Asian J Pharm Clin Res 2015;8:132-5.
12. Gagan G, Tarun G, Basant M, Gaurav C, Goutam R, Amit KG. Development and characterization of niosomal gel for topical delivery of benzoyl peroxide. Drug Deliv 2016;22:1027-42.
13. Susanta P, Mayukh J, Anannya B, Sunirmal B, Joyeeta GR, Puja C. Topical liposomal gel: A new strategy of novel drug delivery. World J Pharm Pharm Sci 2016;6:568-77.
14. Dheeraj N, Nidhi A, Deepshikha K. Evaluation of liposomal gossypin in animal models of epilepsy. Int J Pharm Pharm Sci 2016;8:247-51.
15. Subash C, Pandey VP. Formulation and evaluation of Glimepiride-loaded liposomes by ethanol-injection method. Asian J Pharm Clin Res 2016;9:192-5.
16. Fatima T, Raza M, Shukla AK. Development and characterization of prednisolone liposomal gel for the treatment of rheumatoid arthritis. Int Res J Pharm 2015;6:133-7.
17. Ahmed AN, Ahmed GH, Amina LM, Marwa MM, Nabil YA. Liposomal Microencapsulation of rodent-repelling agents onto Jute Burlaps: Assessment of Cytotoxicity and rat behavioural test. J Appl Pharm Sci 2016;6:142-50.
18. Olga P, Jana S, Zoran K, Vesna R. An overview: Methods for preparation and characterization of liposomes as drug delivery systems. Int J Pharm Phytopharm Res 2013;3:13-20.
19. Amol AT, Arun TP, Milind JU, Darshan RT. Investigation of effect of phospholipids on physical and functional characterization of Paclitaxel liposomes. Int J Pharm Pharm Sci 2017;9:141-6.
20. Cedar HAB, Ketan P, Mandip S. Doxorubicin liposomes as an investigative model to study the skin permeation of nanocarriers. Int J Pharm 2015;489:1-11.
21. Zhengzi Q, Xianhuo W, Zheng S, Huilai Z, Shiyong Z, Jing Z, et al. A Phase I Trial to evaluate the multiple-dose safety and antitumor activity of Ursolic acid liposomes in subjects with advanced solid tumors. Bio Med Res Int 2015;2015:1-7.
22. Srinivas MB, Vishakha K, Prakash P, Jamal BD, Govardhan T, Muni SP. Formulation and in vitro evaluation of liposomes loaded with mupirocin. Int J Res Pharm Nano Sci 2015;4:162-74.
23. Monika B, Szilvia B, Maria BS, Anita K, Erzsebet C. DSC for evaluating the encapsulation efficiency of lidocaine loaded liposomes compared to the ultracentrifugation method. J Therm Anal Calorim 2017;130:1619-25.
24. Eskandar M, Mohsen T, Ali B, Somayeh H. Formulation and in vitro evaluation of topical liposomal gel of triamcinolone acetonide. Res J Pharm Biol Chem Sci 2013;4:101-7.
25. Milla GB, Silvio AG, Camila MD, Larissa AR, Pedro JR, Ferdinando OC, et al. Development and evaluation of stability of a gel formulation containing the Monoterpene Borneol Sci World J 2016;2016:1-4.
26. Panuganti V, Ellutla M, Prasanna RY, Vayalpati AR, Bandugalla SR, Basappa K. Liposomal Aloe vera trans-emulgel drug delivery of naproxen and nimesulide: A study. Int J Pharma Investig 2015;5:28-34.
27. Khalid ME, Fathy IA, Ahmed EL, Abd ES, Alaa EA. Diacereinniosomal gel for topical delivery: Development, in vitro and in vivo assessment. J Lipos Res 2016;26:57-68.
28. Girish S, Seth AK, Ghanshyam P, Sachin C, Ankur J. Formulation and in vitro evaluation of berberine containing liposome optimized by 32 full factorial designs. J Appl Pharm Sci 2015;5:23-8.
29. Sharma NK, Kumar V. Release kinetics of novel photosensitive liposome for triggered delivery of entrapped drug. Int J Pharm Tech Res 2015;8:106-13.
30. Yan L, Ruiyuan L, Jun Y, Yuanjie S, Guanghui M, Zhenzhong Z, et al. Enhanced retention and anti-tumor efficacy of liposomes by changing their cellular uptake and pharmacokinetics behaviour. Biomaterial 2015;41:1-14.
31. Shabnam, Prathima S, Ravindra BD. Formulation and evaluation of parenteral Methotrexate nanoliposomes. Int J Pharm Pharm Sci 2014;6:295-300.
32. Akshay SR, Sudipta D, Arnab S. Design, formulation and evaluation of liposome containing isoniazid. Int J Appl Pharm 2018;10:52-6.
33. Meghana G, Narayana RK, Siddhartha VT, Raviteja G, Saikrishna RC, Ganesh GN. Formulation and evaluation of Tolnaftate loaded topical liposomal gel for effective skin drug delivery to treat fungal diseases. J Chem Pharm Res 2014;6:856-66.
34. Eman SE, Amna MM, Abeer MK, Doaa GH. Nanoemulsion gel of nutraceutical co-enzyme Q10 as an alternative to conventional topical delivery system to enhance skin permeability and antiwrinkle efficiency. Int J Pharm Pharm Sci 2017;9:207-17.
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