FORMULATION AND EVALUATION OF ZIDOVUDINE LOADED OLIBANUM RESIN MICROCAPSULES: EXPLORING THE USE OF NATURAL RESINS AS BIODEGRADABLE POLYMERIC MATERIALS FOR CONTROLLED RELEASE
Abstract
ABSTRACT
The aim of the present study is to develop and evaluate natural biodegradable microcapsules of zidovudine (AZT) by using olibanum resin as microencapsulating agent, which after oral administration could improve the bioavailability of the drug, in order to provide the sustained release to minimize the dose dependent side effects as well as to improve patient compliance. Â An industrially feasible emulsification-solvent evaporation method was used for preparation of different batches of microcapsules. The proposed system was evaluated in vitro for particle morphology, microencapsulation efficiency, production yield, micromeritic properties, release profile and release kinetics etc. Physico-chemical characteristics of AZT and AZT loaded microcapsules were evaluated by differential scanning calorimetry (DSC), X-ray diffraction (XRD), and infrared spectroscopy (FTIR). The resin coated microcapsules were found to be spherical, discrete and free flowing. Microencapsulation efficiency was in a narrow range (81-88%) suggesting an identical distribution of drug in different batches. DSC and XRD results showed a partial modification in AZT's solid state. Zidovudine release from optimized batches of resin coated microcapsules was slow and over 24 hours depending on the core: coat ratio. Drug release was found to be following Fickian diffusion mechanism. The resin coated microcapsules exhibited good controlled release characteristics and were found to be suitable for once a day oral controlled release product.
Â
Downloads
References
REFERENCES
Jantzen GM, Robinson JR, Sustained- and Controlled- Release Drug-Delivery systems, in Modern Pharmaceutics (Banker GS and Rhodes CT, eds.). informa healthcare: USA; 2009. p. 502.
Robinson JR and Lee VHL, (eds.), Controlled drug delivery: Fundamentals and Applications. informa healthcare: USA; 2009. p. 5-6.
Chien YW, Novel Drug Delivery Systems: Oral Drug Delivery and Delivery systems. New York: Marcel Dekker; 1992. p. 141.
Allen LV, Popovich NG, Ansel HC, Ansel’s Pharmaceutical Dosage Forms and Drug Delivery Systems. 9th ed. LIPPINCOTT WILLIAMS & WILKINS: USA; 2011. p 258-259.
Chickering D.E, Mathiowitz E. Bioadhesive microspheres: I. A novel electrobalance- based method to study adhesive interactions between individual microspheres and intestinal mucosa. J Control Rel 1995; 34: 251-261.
Davis SS, Hardy JG, Taylor. MJ, Whalley DR, Wilson CG. A comparative study of gastrointestinal transit of a pellet and tablet formulation. Int J pharm 1984; 21: 167-177.
Follonier N, Doelkar E. Biopharmaceutical comparison of oral multiple unit and single unit sustained release dosage forms. STP Pharm Sci 1992; 2: 141-158.
Burgess DJ and Hickey AJ. Microspheres technology and applications. In: Encyclopedia of pharmaceutical technology. 2nd edn. Marcel Dekker Inc; 2004. 10: p. 1-29.
Kondo A, Eds. In: Microcapsule processing technology, New York: Marcel Dekker Inc; 1979. P. 18.
Gutcho M.H, Eds. In: Micro capsules and micro encapsulation techniques, New Jersy: Noyes Data Corporation; 1976. p. 236.
Bogdansky S. Natural polymers as drug delivery systems, In: Biodegradable polymers as drug delivery systems, Mark Chasin and Robert Langer (eds.) New York: Marcel Dekker Inc; p. 231- 232.
Kokate CK, Purohit AP, Ghokale SB. Pharmacognosy. Nirali prakashan, Pune. 2006; p. 424-435.
Chowdary KPR, Mohapatra P, Murali Krishna MN. Evaluation of olibanum resin as microencapsulating agent for controlled drug delivery. Ind J Pharm Sci 2006; 68(4): 461-464.
Joachim H, Roland B. The effect of particle microstructure on somatostatin release from poly (lactide) microspheres prepared by a W/O/W solvent evaporation method. J Control Rel 1995; 36: 63-71.
Sergio F, Hans PM, Bruno G. Microencapsulation by solvent extraction/evaporation: reviewing the state of the art of microsphere preparation process technology. J Control Rel 2005; 102: 313-332.
Frezzini C, Leao JC, Porter S. Current trends of HIV disease of the mouth. J Oral Pathol Med 2005; 34: 513–531.
Barre-Sinoussi F. HIV: A discovery opening the road to novel scientific knowledge and global health improvement. J Virol 2010; 397: 255 - 259.
Kumari G, Singh RK. Highly Active Antiretroviral Therapy for treatment of HIV/AIDS patients: Current status and future prospects and the Indian scenario. HIV & AIDS Review 2012; 11: 5 – 14.
www.unaids.org/en/dataanalysis/datatools/aidsinfo : accessed on 12-01-2013.
Broder S. The development of antiretroviral therapy and its impact on the HIV-1/AIDS pandemic. Antiviral Res 2010; 85: 1 – 18.
Jose EA, Cihlar T. Current status and challenges of antiretroviral research and therapy. Antiviral Res 2010; 85: 25 – 33.
Warner GC, Debyser Z, Yasuhiro I, Eric FO, Edwards S, Yonemoto W, Buckheit RW, Jose EA, Cihlar T. Novel targets for HIV therapy. Antiviral Res 2008; 80: 251 – 265.
Ojewole E, Mackraj.I, Naidoo P, Govender T. Exploring the use of novel drug delivery systems for antiretroviral drugs, Eur J Pharm Biopharm 2008; 70: 697-710.
Alejandro S, Diego CA, Angel CM. Drug delivery systems in HIV pharmacotherapy: What has been done and the challenges standing ahead. J Control Rel 2009; 138: 2-15.
Kuksal A, Tiwary AK, Jain NK, Jain S. Formulation and In Vitro Evaluation of Extended-release Matrix of Zidovudine: Influence of Combination of Hydrophilic and Hydrophobic Matrix Formers. AAPS Pharm Sci Tech 2006; 7: E1-E9.
Mainardes RM, Gremiao MPD, Brunetti IL, Fonseca LM, Khalil LM. Zidovudine-loaded PLA and PLA-PEG blend nanoparticles: influence of polymer type on phagocytic uptake by polymorphonuclear cells. J Pharm Sci 2009; 98: 257-267.
Carvalho FC, Sarmento VHV, Chiavacci LA, Barbi MS, Gremiao MPD. Development and in vitro evaluation of surfactant systems for controlled release of zidovudine. J Pharm Sci 2009; 99: 2367-2374.
Mandal TK, Tenjarla S. Preparation of biodegradable microcapsules of zidovudine using solvent evaporation: Effect of the modification of aqueous phase. Int J Pharm 1996; 137: 187-197.
Gallo JM, Clark LN, Rubino JT. Pump delivery of Azidothymidine: Potential for constant concentrations and improved brain delivery. J Control Rel 1989; 9: 249-253.
Prakash K, Raju PN, Shanta KK, Lakshmi MN. Preparation and characterization of lamivudine microcapsules using various cellulose polymers. Trop J Pharm Res 2007; 6(4): 841-847.
Trivedi P, Verma AML, Garud N. Preparation and characterization of aceclofenac microspheres. Asian J Pharm. 2008; 2: 110-115.
Jelvehgari M, Nokhodchi A, Rezapour M, Valizadeh H. Effect of formulation and processing variables on the characteristics of tolmetin microspheres prepared by double emulsion solvent diffusion method. Ind J Pharm Sci 2010; 72(1): 72-78.
Bhanja S, Panigrahi BB, Shukla N, Hardel DK, Sudhakar M. Formulation and in vitro evaluation of nicardipine hydrochloride microcapsules AJPCR 2012; 5(3): 60-63.
Rathore S, Ram A. Floating drug delivery system as an approach to increase the gastric retention of methotrexate: Formulation and Evaluation. AJPCR 2013; 6(1): 42-47.
Wu PC, Huang YB, Chang JS, Tsai MI, Tsai YH. Design and evaluation of sustained release microspheres of potassium chloride prepared by Eudragit®. Eur J Pharm Sci 2003; 19: 115-122.
United States Pharmacopoeia, USPNF, 27th ed. USA: US Pharmacopoeial convention, Rockville (MD); Vol.II, 2004. p. 2303-2304.
Ritger PI, Peppas NA. A simple equation for description of solute release II. Fickian and anomalous release from swellable devices. J Control Rel 1987; 5: 37–42.
Mandal T.K., Lopaez-Anaya A., Onyebueke E., Shekleton M. preparation of biodegradable microcapsules containing zidovudine (AZT) using solvent evaporation technique. J Microencapsulation, 1996; 13(3): 257-267.
Araujo AAS, Storpirtis S, Mercuri LP, Carvalho FMS, Santos Filho M, Matos JR. Thermal analysis of the antiretroviral zidovudine (AZT) and evaluation of the compatibility with excipients used in solid dosage forms. Int J Pharm 2003; 260: 303-314.
Gupta R, Pathak K. Optimization studies on floating multiparticulate gastroretentive drug delivery system of famotidine. Drug Dev Ind Pharm 2008; 34: 1201-1208.
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.