Formulation and Evaluation of Polymeric Nanoparticles of an Antiviral Drug for Gastroretention
DOI:
https://doi.org/10.37285/ijpsn.2011.4.4.6Abstract
The aim of present study was to formulate and evaluate nanoparticles of acyclovir by using different hydrophilic polymers. Acyclovir was selected as a suitable drug for gastro-retentive nanoparticles due to its short half life, low bioavailability, high frequency of administration, and narrow absorption window in stomach and upper part of GIT. The nano-precipitation method was used to prepare nanoparticles so as to avoid both chlorinated solvents and surfactants to prevent their toxic effect on the body. Nanoparticles of acyclovir were prepared by using hydrophilic polymers such as bovine serum albumin, chitosan, and gelatin. The prepared formulations were then characterized for particle size, polydispersity index, zeta potential, loading efficiency, encapsulation efficiency and drug-excipient compatibility. The prepared nanoparticulate formulations of acyclovir with different polymers in 1:1 ratio have shown particle size in the range of 250.12-743.07 nm, polydispersity index (PDI) in the range of 0.681-1.0, zeta potential in the range of -14.2 to +33.2 mV, loading efficiency in the range of 8.74-17.54%, and entrapment efficiency in the range of 55.7%-74.2%. Nanoparticulate formulation prepared with chitosan in 1:1 ratio showed satisfactory results i.e. average particle size 312.04 nm, polydispersity index 0.681, zeta potential 33.2 mV, loading efficiency 17.54%, and entrapment efficiency 73.4%. FTIR study concluded that no major interaction occurred between the drug and polymers used in the present study.
Downloads
Metrics
Keywords:
Nanoparticles, gastro-retentive, nano-precipitation, polydispersity index, zeta potential, entrapment efficiency
Downloads
Published
How to Cite
Issue
Section
References
Attia IA, El-Giawy SA, Fouda MA and Donia AM (2007). Influence of a niosomal formulation on the oral bioavailability of acyclovir in rabbits. AAPS Pharm SciTech 8; 106: E1-E27.
Barratt G (1999). Characterization of colloidal drug carrier systems with zeta potential measurements. Pharma Tech Eur 11: 25–32.
Bellare J, Banerjee R and Das S (2005). Aspirin loaded albumin nanoparticles by coacervation: Implications in drug delivery. Trends Bio Artif Organs 18: 203-211.
Dalengon F, Amjaud Y, Lafforgue C, Derouin F, Fessi H (1998). Atovaquone and rifabutine-loaded nanocapsules: Formulation studies. Int J Pharm 153: 127-130.
Deshpande AA, Rhodes TN and Shah H (1996). Controlled release drug delivery systems for prolonged gastric residence an overview. Drug dev Ind pharm 22: 531-539.
Elshafeey AH, Kamel AO and Awad GAS (2010). Ammonium methacrylate unit’s polymer content and their effect on acyclovir colloidal nanoparticles properties and bioavailability in human volunteers. Colloids and Surf B: Biointerfaces 75: 398-404.
Garg R and Gupta GD (2008). Progress in controlled gastroretentive delivery systems. Trop J Pharm Res 7: 1055-1066.
Groning R, Berntgen M and Geogarakis M (1996). Acyclovir serum concentrations following peroral administration of magnetic depot tablets and the influence of extra corporal magnet to control gastrointestinal transit. Eur J Pharm Biopharm 46: 285-91.
Gupta SN and Aggarwal N (2007). A gastro-retentive floating delivery system for 5-Fluorouracil. Asian Journal of Pharmaceutical Sciences 2: 143-149.
Hejazi R and Amiji M (2003). Chitosan-based gastrointestinal delivery systems. J Control Release 89: 151-165.
Hwang SJ, Park H and Park K (1998). Gastric retentive drug delivery systems. Crit Rev Ther Drug 15: 243-248.
Kharia AA, Hiremath SN, Singhai AK, Omray LK, Jain SK (2010). Design and optimization of floating drug delivery system of acyclovir. Indian J Pharm Sci 72: 599-606.
Lueben HL, Lehr CM, Rentel CO, Noach ABJ, Boer AGD, Verhoef JC and Junginger HE (1994). Bioadhesive polymers for the peroral delivery of peptide drugs. J Control Release 29: 329-338
Nidhin M, Indumathy R, Sreeram KJ and Balachandran U (2008). Synthesis of iron oxide nanoparticles of narrow size distribution on polysaccharide templates. Bull Mater Sci 31: 93-96.
O’Brien J and Campoli D (1989). Acyclovir: an updated review of its antiviral activity, pharmacokinetics properties and therapeutic efficacy. Drugs 37: 233-309.
Palmberger TF, Hpmbach J and Schnurch AB (2008). Thiolated chitosan: Development and in vitro evaluation of an oral delivery system for acyclovir. Int J Pharm 348: 54-60.
Park K and Robinson JR (1984). Bioadhesive polymers as platforms for oral-controlled drug delivery: method to study bioadhesion. Int J Pharm 19: 107-127.
Patel JK and Patel MM (2007). Stomach Specific Anti-Helicobacter Pylori Therapy: Preparation and Evaluation of Amoxicillin – Loaded Chitosan Muco adhesive Microspheres. Curr Drug Deliv 4: 41-50.
Pignatello R, Ricupero N, Bucolo, Maugeri F, Maltese A and Puglisi G (2006). Preparation and characterization of eudragit retard nanasuspensions for the ocular delivery of cloricromene. AAPS Pharm SciTech 24; 7: E27.
Rao PB, Kottan NA and Snehith VS (2005). Development of gastroretentive drug delivery system of cephalexin by using factorial design. ARS Pharmaceutica 50: 8-24.
Rouge N, Buri P and Doelke E (1996). Drug absorption sites in the gastrointestinal tract and dosage forms for site specific delivery. Int J Pharm 136:117-139.
Schubert MA and Muller GCC. Solvent injection as a new approach for manufacturing lipid nanoparticles-evaluation of the method and process parameters. Eur J Pharm Biopharm 2003;55:125-131
Shao Z and Mitra AK (1994). Bile salts-fatty acid mixed micelles as nasal absorption promotors: III. Effect on nasal transport and enzymatic degradation of acyclovir prodrug. Pharm Res 11: 243-50.
Singh BN and Kim KH (2000). Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J Control Release 63: 235-239.
Sood A and Panchagnula R (2003). Design of controlled release delivery systems using modified pharmacokinetic approach: a case study for drugs having a short elimination half life and a narrow therapeutic index. Int J Pharm 261: 27-41.
Streubel A, Siepmann J and Bodmeier R (2006). Gastroretentive drug delivery system. Expert Opin Drug Deliv 3: 217-233.
Stulzer HK, Tagliari MP, Parize AL, Silva MAS and Laranjeira MCM (2009). Evaluation of cross-linked chitosan microparticles containing acyclovir obtained by spray-drying. Mater Sci Eng C 29: 387-392.
