Formulation and Evaluation of Gastroretentive Floating Microspheres loaded with Lamivudine
Abstract
Some drugs give poor absorption because of a narrow absorption window in the gastrointestinal tract (GIT). To improve the absorption of such drugs in GIT, gastro retentive drug delivery techniques play a vital role. Lamivudine is an antiviral medicine. The floating gastroretentive microspheres were prepared to attain an extended therapeutic action of Lamivudine. Floating microspheres were formulated to prolong the gastric retention and enhancement of bioavailability of the drug candidate. The floating microspheres were formulated using guar gum and xanthan gum as natural polymers. The proposed floating system was evaluated by preliminary evaluation parameters, micrometric investigation as well as Particle size investigation, Percentage yield of microspheres, Drug entrapment efficiency, In-vitro drug release studies, and their kinetics. The formulated microsphere is evaluated in the form of its stable nature. The formulated microsphere was found to be smooth, spherical, and slightly aggregated containing guar gum whereas xanthan gum containing microsphere was found porous, irregular, grossly, and discrete globular. Formulated microsphere gives a good percentage of drug entrapment and practical yields. The floating microsphere prolonged the drug release by up to 12 hrs. The IR spectroscopy of the prepared formulation was shown that the chemical structure of the Lamivudine was unchanged. The prepared lamivudine microspheres presented gastro retentive and extended-release properties.
Keywords: Lamivudine; Microspheres; Narrow absorption window; Floating system
Keywords:
Lamivudine, Microspheres, Narrow absorption window, Floating systemDOI
https://doi.org/10.22270/jddt.v12i4-S.5462References
Chein YW. Novel drug delivery systems. Marcel jekker Inc., New York. 1992; 13.
Shaha SH, Patel JK, Pundarikakshudu K, Patel NV. An overview of a gastro-retentive floating drug delivery system. Asian journal of pharmaceutical sciences. 2009 Jan; 4(1):65-80.
Sambathkumar R, Venkateswaramurthy N, Vijayabaskaran M, Perumal P. Formulation of clarithromycin loaded mucoadhesive microspheres by emulsification-internal gelation technique for anti-Helicobacter pylori therapy. Int J Pharm Pharm Sci. 2011; 3(2).
Gholap SB, Banarjee SK, Gaikwad DD, Jadhav SL, Thorat RM. Hollow microsphere: A review. International Journal of Pharmaceutical Sciences Review and Research. 2010 Mar; 1(1):74-9.
Ambhore JP, Chaudhari SR, Cheke RS, Kharkar PS. A Concise Analytical Profile of Efavirenz: Analytical Methodologies. Critical Reviews in Analytical Chemistry. 2021 Feb 27:1-0.
Ghosh A, Nayak UK, Roy P. Development, Evaluation and Method selection for the Preparation of lamivudine microspheres. The International Journal of Pharmaceutics. 2007 Jun; 9:67-71.
Singh BN, Kim KH. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. Journal of Controlled release. 2000 Feb 3; 63(3):235-59.
Johnson MA, Moore KH, Yuen GJ, Bye A, Pakes GE. Clinical pharmacokinetics of lamivudine. Clinical pharmacokinetics. 1999 Jan; 36(1):41-66.
van Leeuwen R, Lange JM, Hussey EK, Donn KH, Hall ST, Harker AJ, Jonker P, Danner SA. The safety and pharmacokinetics of a reverse transcriptase inhibitor, 3TC, in patients with HIV infection: a phase I study. AIDS (London, England). 1992 Dec 1; 6(12):1471-5.
Ambhore JP, Adhao VS, Cheke RS, Popat RR, Gandhi SJ. Futuristic review on progress in force degradation studies and stability indicating assay method for some antiviral drugs. GSC Biological and Pharmaceutical Sciences. 2021; 16(1):133-49.
Adhao, V.S., Chaudhari, S.R., Ambhore, J.P., Sangolkar, S., Thenge, R.R., Cheke, R.S. and Patil, A.S., Reverse phase-liquid chromatography assisted protocol for simultaneous determination of lamivudine and tenofovir disoproxil fumarate in combined medication used to control HIV infection: an investigative approach. Future Journal of Pharmaceutical Sciences, 2021; 7(1):1-11.
Wonganan P, Limpanasithikul W, Jianmongkol S, Kerr SJ, Ruxrungtham K. Pharmacokinetics of nucleoside/nucleotide reverse transcriptase inhibitors for the treatment and prevention of HIV infection. Expert Opinion on Drug Metabolism & Toxicology. 2020 Jul 2; 16(7):551-64.
Prakash K, Raju PN, Shanta KK, Lakshmi MN. Preparation and characterization of lamivudine microcapsules using various cellulose polymers. Tropical Journal of Pharmaceutical Research. 2007 Dec 19; 6(4):841-7.
Cheke RS, Shinde SD, Ambhore JP, Chaudhari SR, Bari SB. Quinazoline: An update on current status against convulsions. Journal of Molecular Structure. 2022 Jan 15; 1248:131384.
A Swarna Kumari, B Siddhartha, K Manasa Bhanu, N Sai Ram, S Manohar, T PoornaSantosh Kumar, V Swarupa Rani, Balaji Maddiboyina. Formulation and Evaluation of floating tablets of Antiretroviral drug Lamivudine. ijamscr [Internet]. 2021Sep.1 [cited 2022Jun.18]; 9(3):507-13.
Negi P, Cheke RS, Patil VM. Recent advances in pharmacological diversification of Src family kinase inhibitors. Egyptian Journal of Medical Human Genetics. 2021 Dec; 22(1):1-6.
Singh B, Garg B, Chaturvedi SC, Arora S, Mandsaurwale R, Kapil R, Singh B. Formulation development of gastroretentive tablets of lamivudine using the floating-bioadhesive potential of optimized polymer blends. Journal of Pharmacy and Pharmacology. 2012 May; 64(5):654-69.
Cheke RS, Patel HM, Patil VM, Ansari IA, Ambhore JP, Shinde SD, Kadri A, Snoussi M, Adnan M, Kharkar PS, Pasupuleti VR. Molecular Insights into Coumarin Analogues as Antimicrobial Agents: Recent Developments in Drug Discovery. Antibiotics. 2022 May; 11(5):566.
Desi Reddy RB, Malleswari K, Prasad G, Prasanna D. Preparation and in vitro evaluation of lamivudine floating sodium alginate beads. International Journal of Pharmaceutical and Clinical Research. 2012; 4(4):81-8.
Patel KS, Patel MB. Preparation and evaluation of chitosan microspheres containing nicorandil. International journal of pharmaceutical investigation. 2014 Jan; 4(1):32.
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