Login Register Cart 0
Generic placeholder image

Current Applied Polymer Science

Editor-in-Chief

ISSN (Print): 2452-2716
ISSN (Online): 2452-2724

Back
Journal Home About Journal Editorial Board Journal Insight Current Issue Volumes/Issues
Subscribe
Research Article

Clarithromycin Loaded Chitosan Nanoparticles: Development and Characterization

Author(s): Ashvini Herimatha*, Shivanand K Mutta, Anirbandeep Bose and Anudeep Balla

Volume 4, Issue 1, 2021

Published on: 29 October, 2020

Page: [55 - 71] Pages: 17

DOI: 10.2174/2452271604999201029195547

Price: $65

Abstract

Background: Chitosan nanoparticles have been extensively studied and used due to their well-recognized applicability in various fields. Chitosan, a natural polysaccharide polymer, is extensively used in pharmaceuticals to deliver a wide variety of therapeutic agents. Chitosan is a biocompatible and biodegradable mucoadhesive polymer that has been extensively used in the preparation of multi particles, particularly nano- and microparticles.

Objective: The main aim of the present study was to optimize the conditions for the preparation of chitosan nanoparticles to get optimal particle size, with optimal zeta potential and narrow polydispersity index and anti-bacterial activity.

Methods: Include the ionic gelation technique for chitosan nanoparticle preparation. The influence of formulation parameters and process parameters on the chitosan nanoparticles were investigated. Besides, the suspension stability of the prepared nanoparticles was also assessed on storage at 4°C.

Results: The formulation and process parameters showed a significant effect on the physicochemical and morphological characteristics of the chitosan nanoparticles. The chitosan nanoparticles prepared under optimum conditions (chitosan concentration of 0.5% w/v, CS: TPP mass ratio of 1:3, initial pH of chitosan solution of 4.5, stirred at 750 rpm for 30 min) had shown a mean particle size of ~326.8±15 nm, zeta potential of +28.2 ± 0.5 mV, and PDI of 0.21 ± 0.02. The encapsulation of the clarithromycin slightly increased the polydispersity index, but the zeta potential of the unloaded nanoparticles was not affected while the particle size increased. Under optimum conditions, clarithromycin encapsulation efficiency into nanoparticles was found to be 70%. Additionally, chitosan- tripolyphosphate nanoparticles were shown to be stable for a minimum of fifteen days in deionized water at 4°C.

Conclusion: The current study concludes the optimal conditions to formulate the chitosan nanoparticles with optimal physicochemical characteristics.

Keywords: Chitosan nanoparticles, formulation parameters, process parameters, particle size, polydispersity index, zeta potential.

« Previous Next »
Graphical Abstract

[1]
Sahoo SK, Labhasetwar V. Nanotech approaches to drug delivery and imaging. Drug Discov Today 2003; 8(24): 1112-20.
[http://dx.doi.org/10.1016/S1359-6446(03)02903-9] [PMID: 14678737]
[2]
Peer D, Karp JM, Hong S, Farokhzad OC, Margalit R, Langer R. Nanocarriers as an emerging platform for cancer therapy. Nat Nanotechnol 2007; 2(12): 751-60.
[http://dx.doi.org/10.1038/nnano.2007.387] [PMID: 18654426]
[3]
Couvreur P, Vauthier C. Nanotechnology: Intelligent design to treat complex disease. Pharm Res 2006; 23(7): 1417-50.
[http://dx.doi.org/10.1007/s11095-006-0284-8] [PMID: 16779701]
[4]
Armstead AL, Li B. Nanomedicine as an emerging approach against intracellular pathogens. Int J Nanomedicine 2011; 6: 3281-93.
[PMID: 22228996]
[5]
Lozano R, Naghavi M, Foreman K, et al. Global and regional mortality from 235 causes of death for 20 age groups in 1990 and 2010: A systematic analysis for the Global Burden of Disease Study 2010. Lancet 2012; 380(9859): 2095-128.
[http://dx.doi.org/10.1016/S0140-6736(12)61728-0] [PMID: 23245604]
[6]
Eleraky NE, Allam A, Hassan SB, Omar MM. Nanomedicine fight against antibacterial resistance: An overview of the recent Pharmaceutical innovations. Pharmaceutics 2020; 12(2): 1-51.
[http://dx.doi.org/10.3390/pharmaceutics12020142] [PMID: 32046289]
[7]
Peters DH, Clissold SP. Clarithromycin. A review of its antimicrobial activity, pharmacokinetic properties and therapeutic potential. Drugs 1992; 44(1): 117-64.
[http://dx.doi.org/10.2165/00003495-199244010-00009] [PMID: 1379907]
[8]
Langtry HD, Brogden RN. Clarithromycin. A review of its efficacy in the treatment of respiratory tract infections in immunocompetent patients. Drugs 1997; 53(6): 973-1004.
[http://dx.doi.org/10.2165/00003495-199753060-00006] [PMID: 9179528]
[9]
Salem II, Düzgünes N. Efficacies of cyclodextrin-complexed and liposome-encapsulated clarithromycin against Mycobacterium avium complex infection in human macrophages. Int J Pharm 2003; 250(2): 403-14.
[http://dx.doi.org/10.1016/S0378-5173(02)00552-5] [PMID: 12527166]
[10]
Lohitnavy M, Lohitnavy O, Wittaya-areekul S, Sareekan K, Polnok S, Chaiyaput W. Average bioequivalence of clarithromycin immediate released tablet formulations in healthy male volunteers. Drug Dev Ind Pharm 2003; 29(6): 653-9.
[http://dx.doi.org/10.1081/DDC-120021314] [PMID: 12889783]
[11]
Whitman MS, Tunkel AR. Azithromycin and clarithromycin: Overview and comparison with erythromycin. Infect Control Hosp Epidemiol 1992; 13(6): 357-68.
[http://dx.doi.org/10.2307/30147135] [PMID: 1320067]
[12]
Liu H, Du Y, Wang X, Sun L. Chitosan kills bacteria through cell membrane damage. Int J Food Microbiol 2004; 95(2): 147-55.
[http://dx.doi.org/10.1016/j.ijfoodmicro.2004.01.022] [PMID: 15282127]
[13]
Vishu Kumar AB, Varadaraj MC, Gowda LR, Tharanathan RN. Low molecular weight chitosans preparation with the aid of pronase, characterization and their bactericidal activity towards Bacillus cereus and Escherichia coli. Biochim Biophys Acta 2007; 1770(4): 495-505.
[http://dx.doi.org/10.1016/j.bbagen.2006.12.003] [PMID: 17240531]
[14]
Piras AM, Maisetta G, Sandreschi S, et al. Preparation, physical-chemical and biological characterization of chitosan nanoparticles loaded with lysozyme. Int J Biol Macromol 2014; 67: 124-31.
[http://dx.doi.org/10.1016/j.ijbiomac.2014.03.016] [PMID: 24661890]
[15]
Piras AM, Maisetta G, Sandreschi S, et al. Chitosan nanoparticles loaded with the antimicrobial peptide temporin B exert a long-term antibacterial activity in vitro against clinical isolates of Staphylococcus epidermidis. Front Microbiol 2015; 6: 372.
[http://dx.doi.org/10.3389/fmicb.2015.00372] [PMID: 25972852]
[16]
Sobhani Z, Mohammadi Samani S, Montaseri H, Khezri E. Nanoparticles of chitosan loaded ciprofloxacin: Fabrication and antimicrobial activity. Adv Pharm Bull 2017; 7(3): 427-32.
[http://dx.doi.org/10.15171/apb.2017.051] [PMID: 29071225]
[17]
Alqahtani FY, Aleanizy FS, Tahir EE, et al. Preparation, characterization, and antibacterial activity of diclofenac-loaded chitosan nanoparticles. Saudi Pharm J 2019; 27(1): 82-7.
[http://dx.doi.org/10.1016/j.jsps.2018.08.001] [PMID: 30662310]
[18]
Mirnejad R, Jahromi M, Al-Musawi S, et al. Curcumin-loaded chitosan tripolyphosphate nanoparticles as a safe, natural and effective antibiotic inhibits the infection of Staphylococcus aureus and Pseudomonas aeruginosa in vivo . Iranian J Biotechnol 2014; 12(3): 1-8.
[http://dx.doi.org/10.15171/ijb.1012]
[19]
Ibrahim HM, El-Bisi MK, Taha GM, El-Alfy EA. Chitosan nanoparticles loaded antibiotics as drug delivery biomaterial. J Appl Pharm Sci 2015; 5(10): 85-90.
[http://dx.doi.org/10.7324/JAPS.2015.501015]
[20]
Takahashi C, Asaka T, Akachi Y, et al. Morphological study of efficacy of clarithromycin-loaded nanocarriers for treatment of biofilm infection disease. Med Mol Morphol 2016.
[PMID: 27119723]
[21]
Golmohamadi M, Ghorbani HR, Otadi M. Synthesis of chitosan nanoparticles loaded with antibiotics as drug carriers and the study of antibacterial activity. J Nanoana 2019; 6(1): 72-9.
[22]
Fazil M, Md S, Haque S, et al. Development and evaluation of rivastigmine loaded chitosan nanoparticles for brain targeting. Eur J Pharm Sci 2012; 47(1): 6-15.
[http://dx.doi.org/10.1016/j.ejps.2012.04.013] [PMID: 22561106]
[23]
Shanmuga SS, Rekha B, Sridhar S, Sangeetha D. Fabrication of chitosan/TPP nanoparticles as a carrier towards the treatment of cancer. Int J Drug Deliv 2013; 5: 35-42.
[24]
Calvo P, Remunan-Lopez C, Vila-Jato JL, Alonso MJ. Novel hydrophilic chitosan-polyethylene oxide nanoparticles as protein carriers. J Appl Polym Sci 1997; 63: 125-32.
[http://dx.doi.org/10.1002/(SICI)1097-4628(19970103)63:1<125::AID-APP13>3.0.CO;2-4]
[25]
Esmaeili F, Atyabi F, Dinarvand R. Preparation and characterization of Estradiol-loaded PLGA nanoparticles using homogenization-solvent diffusion method. Daru 2008; 16(4): 196-202.
[26]
Avadi MR, Sadeghi AM, Mohammadpour N, et al. Preparation and characterization of insulin nanoparticles using chitosan and Arabic gum with ionic gelation method. Nanomedicine (Lond) 2010; 6(1): 58-63.
[http://dx.doi.org/10.1016/j.nano.2009.04.007] [PMID: 19447202]
[27]
Wang X, Chi N, Tang X. Preparation of estradiol chitosan nanoparticles for improving nasal absorption and brain targeting. Eur J Pharm Biopharm 2008; 70(3): 735-40.
[http://dx.doi.org/10.1016/j.ejpb.2008.07.005] [PMID: 18684400]
[28]
Harsha S, R C, Rani S. Ofloxacin targeting to lungs by way of microspheres. Int J Pharm 2009; 380(1-2): 127-32.
[http://dx.doi.org/10.1016/j.ijpharm.2009.07.020] [PMID: 19646516]
[29]
Indian Pharmacopiea. Government of India, Ministry of Health and Family Welfare. Indian Pharmacopeia Commission, Ghaziabad 6th ed 1: 563.
[30]
Shoaib MH, Tazeen J, Merchant HA, Yousuf RI. Evaluation of drug release kinetics from ibuprofen matrix tablets using HPMC. Pak J Pharm Sci 2006; 19(2): 119-24.
[PMID: 16751122]
[31]
Gautam S, Mahaveer S. In vitrodrug release characterization models. Int J Pharm Res 2011; 2(1): 77-84.
[32]
Bangale GS, Shinde GV, Rajesh KS. Formulation and optimization of nanoparticale by 32 factorial design for colon targeting. Glob J Pharmaceu Sci 2019; 7(1): 1-15.
[33]
Methods for dilution antimicrobial susceptibility tests for bacteria that grow aerobically. Wayne, PA: National Committee for Clinical Laboratory Standards. 2000.
[34]
Baurer AW Kirby, Sherris JC, Turck M. Antibiotic susceptibility testing by a standardized disk method. American J Clion Path 1996; 45(4): 493-6.
[35]
Wani IA, Khatoon S, Ganguly A, Ahmed J, Ahmad T, Manzoor N. Structural characterization and antimicrobial properties of silver nanoparticles prepared by inverse microemulsion method. Colloids Surf B Biointerfaces 2013; 101: 243-50.
[http://dx.doi.org/10.1016/j.colsurfb.2012.07.001] [PMID: 23010026]
[36]
Raja MA, Katas H, Jing Wen T. Stability, intracellular delivery, and release of siRNA from chitosan nanoparticles using different cross-Linkers. PLoS One 2015; 10(6): e0128963.
[http://dx.doi.org/10.1371/journal.pone.0128963] [PMID: 26068222]
[37]
Gan Q, Wang T, Cochrane C, McCarron P. Modulation of surface charge, particle size and morphological properties of chitosan-TPP nanoparticles intended for gene delivery. Colloids Surf B Biointerfaces 2005; 44(2-3): 65-73.
[http://dx.doi.org/10.1016/j.colsurfb.2005.06.001] [PMID: 16024239]
[38]
Fan W, Yan W, Xu Z, Ni H. Formation mechanism of monodisperse, low molecular weight chitosan nanoparticles by ionic gelation technique. Colloids Surf B Biointerfaces 2012; 90: 21-7.
[http://dx.doi.org/10.1016/j.colsurfb.2011.09.042] [PMID: 22014934]
[39]
Hu B, Pan C, Sun Y, Hou Z, Ye H, Zeng X. Optimization of fabrication parameters to produce chitosan-tripolyphosphate nanoparticles for delivery of tea catechins. J Agric Food Chem 2008; 56(16): 7451-8.
[http://dx.doi.org/10.1021/jf801111c] [PMID: 18627163]
[40]
Liu H, Gao C. Preparation and properties of ionically cross-linked chitosan nanoparticles. Polym Adv Technol 2009; 20: 613-9.
[http://dx.doi.org/10.1002/pat.1306]
[41]
Qun G, Ajun W. Effects of molecular weight, degree of acetylation and ionic strength on surface tension of chitosan in dilute solution. Carbohydr Polym 2006; 64: 29-36.
[http://dx.doi.org/10.1016/j.carbpol.2005.10.026]
[42]
Zahid H, Shariza S. Preparation, characterisation and colloidal stability of chitosan- tripolyphosphate nanoparticles: Optimisation of formulation and process parameters. Int J Pharm Pharm Sci 2016; 8(3): 297-308.
[43]
Zhu HJ, Liu XM, Yangn H, Shen XD. Effect of the stirring rate on physical and electrochemical properties of LiMnPO4 nanoplates prepared in a polyol process. Ceram Interfaces 2014; 40: 6699-704.
[http://dx.doi.org/10.1016/j.ceramint.2013.11.131]
[44]
Nazeri N, Avadi MR, Faramarzi MA, et al. Effect of preparation parameters on ultra low molecular weight chitosan/hyaluronic acid nanoparticles. Int J Biol Macromol 2013; 62: 642-6.
[http://dx.doi.org/10.1016/j.ijbiomac.2013.09.041] [PMID: 24099942]
[45]
Hassani S, Laouini A, Fessi H, Charcosset C. Preparation of chitosan-TPP nanoparticles using microengineered membranes–Effect of parameters and encapsulation of tacrine. Colloids Surf A Physicochem Eng Asp 2015; 482: 34-43.
[http://dx.doi.org/10.1016/j.colsurfa.2015.04.006]
[46]
Wu Y, Yang W, Wang C, Hu J, Fu S. Chitosan nanoparticles as a novel delivery system for ammonium glycyrrhizinate. Int J Pharm 2005; 295(1-2): 235-45.
[http://dx.doi.org/10.1016/j.ijpharm.2005.01.042] [PMID: 15848008]
[47]
Mohanraj VJ, Chen Y. Nanoparticles – a review. Trop J Pharm Res 2006; 5: 561-73.
[48]
Meng J, Sturgis TF, Youan BB. Engineering tenofovir loaded chitosan nanoparticles to maximize microbicide mucoadhesion. Eur J Pharm Sci 2011; 44(1-2): 57-67.
[http://dx.doi.org/10.1016/j.ejps.2011.06.007] [PMID: 21704704]
[49]
Yu CY, Cao H, Zhang XC, et al. Hybrid nanospheres and vesicles based on pectin as drug carriers. Langmuir 2009; 25(19): 11720-6.
[http://dx.doi.org/10.1021/la901389v] [PMID: 19719161]
[50]
Mainardes RM, Evangelista RC. PLGA nanoparticles containing praziquantel: Effect of formulation variables on size distribution. Int J Pharm 2005; 290(1-2): 137-44.
[http://dx.doi.org/10.1016/j.ijpharm.2004.11.027] [PMID: 15664139]
[51]
Fonseca C, Simões S, Gaspar R. Paclitaxel-loaded PLGA nanoparticles: Preparation, physicochemical characterization and in vitroanti-tumoral activity. J Control Release 2002; 83(2): 273-86.
[http://dx.doi.org/10.1016/S0168-3659(02)00212-2] [PMID: 12363453]
[52]
Tripathi R, Gupta SA. Saraf. PLGA nanoparticles of antitubercular drug: Drug loading and release studies of a water in-soluble drug. Int J Pharm Tech Res 2010; 2: 2116-23.
[53]
Hadipour MP, Ramezani V, Esfandi E. Development of a nano–micro carrier system for sustained pulmonary delivery of clarithromycin. Powder Technol 2013; 239: 478-83.
[http://dx.doi.org/10.1016/j.powtec.2013.02.025]
[54]
Dash M, Chiellini F, Ottenbrite RM, Chiellini E. Chitosan-A versatile semi-synthetic polymer in biomedical applications. Prog Polym Sci 2011; 36(8): 981-1014.
[http://dx.doi.org/10.1016/j.progpolymsci.2011.02.001]
[55]
Mohammadi G, Nokhodchi A, Barzegar-Jalali M, et al. Physicochemical and anti-bacterial performance characterization of clarithromycin nanoparticles as colloidal drug delivery system. Colloids Surf B Biointerfaces 2011; 88(1): 39-44.
[http://dx.doi.org/10.1016/j.colsurfb.2011.05.050] [PMID: 21752610]
[56]
Tsai ML, Chen RH, Bai SW, Chen WY. The storage stability of chitosan/tripolyphosphate nanoparticles in a phosphate buffer. Carbohydr Polym 2011; 84: 756-61.
[http://dx.doi.org/10.1016/j.carbpol.2010.04.040]

Rights & Permissions Print Cite
Article Metrics
27
1
© 2024 Bentham Science Publishers | Privacy Policy