Microsponge based drug delivery system of voriconazole for fungal infection: formulation development and In-vitro evaluation
The plan behind the present research work was to develop a microsponge based dosage form for modified delivery of voriconazole prepared by quasi-emulsion solvent diffusion method using polymer Ethylcellulose with two factors drug-polymer ratios and surfactant concentration, these two factors influences micro particles and physical properties. The characterization techniques followed for the formed microsponges were DSC, FT-IR, SEM and particle size analysis, along with morphology, drug loading, in-vitro drug release data. DSC and FT-IR data discloses that there were no chemical interactions between drug and polymer used. The drug-polymer ratio and surfactant concentration showed notable impact on drug content, encapsulation efficiency and particle size, SEM micrographs revealed that microsponges formed were spherical in shape with porous surface, and had 119.47 μm mean particle size. The microsponges were then loaded in carbopol gel followed by ex vivo drug deposition, primary skin irritancy study, in vivo antibacterial activity and in-vitro drug release study; which depicted that microsponges with drug-polymer ratio of 1:3 were more capable to give extended drug release of 93.79.±0.06 % at the end of 24 h, better in contrast to conventional formulation. Hence, the developed microsponge based formulation of voriconazole would be a hopeful, promising alternate to conventional therapy for the fungal treatment.
Keywords: Voriconazole, Microsponge, Particle size, Entrapment efficiency, ex vivo drug deposition primary skin irritancy
2. Saroj Kumar Pradhan. Microsponges as the versatile tool for drug delivery system. International Journal of Research in Pharmacy and Chemistry 2011; 1(2):243-258.
3. Kawashima Y, Niwa T, Takeuchi H, Hino T, Ito Y. Control of Prolonged Drug Release and Compression Properties of Ibuprofen Microsponges with Acrylic Polymer, Eudragit RS, by changing their intra particle porosity. Chemical & Pharmaceutical bulletin 1992; 40(1):196-201.
4. Dsouza JI, Masvekar RR, Pattekari PP, Pudi SR, More HN : Microspongic Delivery of Fluconazole for Topical Application. 1st Indo-Japanese International Conference on Advances in Pharmaceutical Research and Technology, Mumbai, India 2005: pp25-29.
5. Topical anti-inflammatory gels of fluocinolone acetonide entrapped in eudragit based microsponge delivery system Res. J. Pharm. Technol., 1 2008, 502-506
6. L.K. Vyas, K.K. Tapar, B.H. Laddha, A.O. Lahoti, R.K.Nema Formulation and development of anti-blemish preparations using microsponge technology J. Chem. Pharm. Res, 2010; 2:562-571
7. Vyas, S.P. Khar R.K. Targeted and Controlled Drug Delivery-Novel Carrier System 1st ed.; CBS Publication: New Delhi 2002
8. Won, R 1987. Method for delivering an active ingredient by controlled time release utilizing a novel delivery vehicle which can be prepared by a process utilizing the active ingredient as a porogen. U.S. Patent 4,690,825 Sep 1,1987.
9. B. V. Mitkari, S. A. Korde, K. R. Mahadik, and C. R. Kokare, “Formulation and evaluation of topical liposomal gel for fluconazole,” Indian Journal of Pharmaceutical Education and Research, 2010; 44(4):324–333.
10. Orlu M, Cevher E, Araman A. Design and evaluation of colon specific drug delivery system containing flurbiprofen microsponges. International Journal of Pharmaceutics Volume 2006 ; 318:103–17
11. Kilicarslan, M., Baykara, T., The effect of the drug/polymer ratio on the properties of verapamil hydrochloride loaded microspheres. Int. J. Pharm, 2003; 252:99–109
12. Nokhodchi, A., Jelvehgari, M., Reza, S.M., Reza, M.M. Factors affecting the morphology of benzoyl peroxide microsponges. Micron 2007; 38:834–840
13. Li SS, Li GF, Liu L, Jiang X, Zhang B, Liu ZG, Li XL, Weng LD, Zuo T, Liu Q. Evaluation of paeonol skin-target delivery from its microsponge formulation: in vitro skin permeation and in vivo microdialysis. PLoS One, 2013; 20, 8(11)1-8.
14. Maiti S., Ray S., Kaity S. Development and evaluation of xanthan gum-facilitated ethyl cellulose microsponges for controlled percutaneous delivery of diclofenac sodium. Acta Pharm, 2011; 61:257–270.
15. Chaudhary H, Rohilla A, Rathee P and Kumar V. Optimization and formulation design of carbopol loaded Piroxicam gel using novel penetration enhancers. Int J Biol Macromol 2013; 55:246-253.
16. V.Thanda, S. Firoz, C. Yerram,A.Vikram, S. K. Divya, andK.T.Murali, Design and characterisation sustained release matrixtablets of Repaglinide using natural polymers, International Journal of Pharmacy, 2012; 2(2):73-83
17. Maheshwari R, Tekade R, Sharma P, Darwhekar G, Tyagi A, Patel R,Jain D Ethosomes and ultra-deformable liposomes for transdermal delivery of clotrimazole: a comparative assessment. Saudi Pharm J, 2012; 20:161–170
18. Saboji JK, Manvi FV, Gadad AP, Patel BD. Formulation and evaluation of ketoconazole microsponge gel by quasi‑emulsion solvent diffusion. J Cell Tissue Res, 2011; 11:2691‑2696.
19. McRipley R, Whitney R Characterization and quantitation ofexperimental surgical-wound infections used to evaluate topical antibacterial agents. Antimicrob Agents Chemother, 1976; 10,38–44
20. Jessup C. J. et al Antifungal Susceptibility Testing of Dermatophytes: Establishing a Medium for Inducing Conidial Growth and Evaluation of Susceptibility of Clinical Isolates. Journal of clinical microbiology, 2000; 38 (1):341–344.
21. K. Westesen, H. Bunjes, and M. H. J. Koch, Physicochemical characterization of lipid nanoparticles and evaluation of theirdrug loading capacity and sustained release potential,” Journal of Controlled Release, 1997; 48(2-3):223–236,
22. Sibel Bozdag Pehlivan, Birsel Subasi, Imran Vural, Nursen Unlu and Yilmaz capan. Evaluation of drug-excipient interaction in the formulation of celecoxib tablets. Acta Poloniae Pharmaceutical Drug Research 2011; 68(3):423-433
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