DEVELOPMENT AND EVALUATION OF RITONAVIR MUCOADHESIVE MICROSPHERES
Abstract
Â
 Objective: The objective of this research was to formulate and evaluate guar gum and ethyl cellulose mucoadhesive microspheres in combination with sodium alginate for controlled release of ritonavir.
Materials and Methods: Microspheres were prepared by ionotropic gelation method using aluminum sulfate as a cross-linking agent. The developed ritonavir microspheres were characterized for micrometrics properties, morphology, drug entrapment efficiency, mucoadhesive property, in vitro drug release and interaction studies (Fourier transforms infrared spectroscopy [FTIR] and differential scanning calorimeter [DSC]).
Results: The ritonavir mucoadhesive microspheres were free-flowing and discrete. The mean particle size ranged from 802.40±3.90 to 962.77±3.16 μm and the entrapment efficiencies ranged from 75.21 to 94.00%. All the ritonavir microsphere batches showed good in vitro mucoadhesive property ranging from 12 to 49% in the in-vitro wash off test. FTIR studies indicated the lack of ritonavir-polymer interactions in the ideal formulation F8. There were no compatibility issues and the crystallinity of ritonavir was found to be reduced in prepared mucoadhesive microspheres, which were confirmed by DSC and X-ray diffraction studies. Among different formulations, the ritonavir microspheres of batch F8 had shown the optimum percent drug entrapment of microspheres and the controlled release of the ritonavir for about 12 hrs. Release pattern of ritonavir from F8 microspheres batch followed Korsmeyers-Peppas and zero-order release kinetic model. The value of ‘n' was found to be 1.593, which indicates that the drug release was followed super Case-II transport type. Stability studies were carried out for F8 formulation at 4°C/ambient, 25±2°C/60±5%, 40±2°C/75±5% relative humidity revealed that the drug entrapment and mucoadhesive behavior were within permissible limits.
Conclusion: The results obtained in this present work demonstrate the potential use of ethyl cellulose polymer for preparation of controlled delivery ritonavir mucoadhesive microspheres and prolonged residence at the absorption site.
Keywords: Guar gum, Ethyl cellulose, Mucoadhesive microspheres, Ritonavir
Downloads
References
Kurana S, Madav NV. Mucoadhesive drug delivery; mechanism and method of evaluation. Int J Pharm Bio Sci 2011;2(1):458-67.
Yellanki SK, Singh J, Syed JA, Bigala R, Goranti S, Nerella NK. Design and characterization of amoxicillin trihydrate mucoadhesive microspheres for prolonged gastric retention. Int J Pharm Sci Drug Res 2010;2(2):112-4.
Chakraborty S, Dinda SC, Patra N, Khandai M. Fabrication and characterization of algino-carbopol microparticulate system of aceclofenac for oral sustained drug delivery. Int J Pharm Sci Rev Res 2010;4(2):192-9.
Sachan NK, Bhattacharya A. Basics and therapeutic potential of oral mucoadhesive microparticulate drug delivery systems. Int J Pharm Clin Res 2009;1:10-4.
Chowdary KP, Rao YS. Mucoadhesive microspheres for controlled drug delivery. Biol Pharm Bull 2004;27(11):1717-24.
6. Garg A, Upadhyay P. Mucoadhesive microspheres: A short review. Asian J Pharm Clin Res 2012;5(3):24-7.
Velmurugan S, Ali M, Kumar P. Microparticulate drug carriers: A promising approach for the delivery of anti HIV drugs. Int J Pharm Pharm Sci 2014;6(2):31-9.
Kenneth N, Parthasarathy V, Manavalan R, Narendra C. ???. Am J PharmTech Res 2012;2(6):231-44.
Velmurugan S, Ali MA. Formulation and evaluation of maraviroc mucoadhesive microsheres by ionotropic gelation method.Int J Pharm Pharm Sci 2013;5:294-302.
Prasant R, Amitava G, Udaya N. Nayak B. Effect of method of preparation on physical properties and in vitro drug release profile of losartan microspheres – A comparative study. Int J Pharm Pharm Sci 2009;1(1):108-18.
Gohel MC, Amin AF. Formulation optimization of controlled release diclofenac sodium microspheres using factorial design. J Control Release 1998;51(2-3):115-22.
Desai S, Vidyasagar G, Shah V, Desa D. Preparation and in vitro characterisation of mucoadhesive microspheres of midazolam: Nose to brain administration. Asian J Pharm Clin Res 2011;4(1):100-02.
Velmurugan S, Ali MA. Mucoadhesive microspheres - An overview. Int J Drug Dev Res 2013;5(3):229-33.
Velmurugan S, Ali MA. Formulation and evaluation of ritonavir mucoadhesive microspheres. Int J Chem Pharm Res 2014;6(5):952-60.
Setter SM, Iltz JL, Thams J, Campbell RK. Metformin hydrochloride in the treatment of type 2 diabetes mellitus: A clinical review with a focus on dual therapy. Clin Ther 2003;25(12):2991-3026.
Ibrahm VT, Senthil Kumar B, Parthiban KG, Manivannan R. Novel drug delivery system; formulation and characterization of exemestane microspheres by chemical cross linking method. Res J Pharm Biol Chem Sci 2010;1(4):83-90.
Arya RK, Juyal V, Singh RD. Development and evaluation of gastro resistant microsphere of pantoprazole. Int J Pharm Pharm Sci 2010;2(3):112-6.
Gangurde HH, Chavan NV, Mundada AS, Derle DV, Tamizharasi S. Biodegradable chitosan-based ambroxol hydrochloride microspheres: Effect of cross-linking agents. J Young Pharm 2011;3(1):9-14.
Pachuau L, Sarkar S, Mazumder B. Formulation and evaluation of matrix microspheres for simultaneous delivery of salbutamol sulphate and theophylline. Trop J Pharm Res 2008;7(2):995-1002.
Martin A. Physical Pharmacy and Physical Chemical Principals in Pharmaceutical Sciences. 4th ed. Baltimore, Maryland: Williams & Wilkins; 1996. p. 427-9.
Published
How to Cite
Issue
Section
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.