title: Development of oral sustained release rifampicin loaded chitosan nanoparticles by design of experiment.
abstract: Objective. The main objective of the present investigation was to develop and optimize oral sustained release Chitosan nanoparticles (CNs) of rifampicin by design of experiment (DOE). Methodology. CNs were prepared by modified emulsion ionic gelation technique. Here, inclusion of hydrophobic drug moiety in the hydrophilic matrix of polymer is applied for rifampicin delivery using CN. The 2(3) full-factorial design was employed by selecting the independent variables such as Chitosan concentration (X 1), concentration of tripolyphosphate (X 2), and homogenization speed (X 3) in order to achieve desired particle size with maximum percent entrapment efficiency and drug loading. The design was validated by checkpoint analysis, and formulation was optimized using the desirability function. Results. Particle size, drug entrapment efficiency, and drug loading for the optimized batch were found to be 221.9 nm, 44.17 ± 1.98% W/W, and 42.96 ± 2.91% W/W, respectively. In vitro release data of optimized formulation showed an initial burst followed by slow sustained drug release. Kinetic drug release from CNs was best fitted to Higuchi model. Conclusion. Design of Experiment is an important tool for obtaining desired characteristics of rifampicin loaded CNs. In vitro study suggests that oral sustained release CNs might be an effective drug delivery system for tuberculosis.
authors.affiliation: Department of Pharmaceutics and Pharmaceutical Technology, Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology, CHARUSAT Campus, Petlad, Anand, Gujarat 388421, India.
authors.forename: Bhavin K
authors.initials: BK
authors.lastname: Patel
authors.forename: Rajesh H
authors.initials: RH
authors.lastname: Parikh
authors.forename: Pooja S
authors.initials: PS
authors.lastname: Aboti
references.citation: J Drug Target. 2004 Feb;12(2):65-70
references.pmid: 15203899
references.citation: Eur J Pharm Sci. 2001 May;13(2):123-33
references.pmid: 11297896
references.citation: Expert Opin Drug Deliv. 2008 Dec;5(12):1323-34
references.pmid: 19040395
references.citation: Drug Discov Today Technol. 2005 Spring;2(1):75-81
references.pmid: 24981758
references.citation: Int J Pharm. 2002 Nov 6;248(1-2):51-60
references.pmid: 12429459
references.citation: Nanomedicine. 2010 Feb;6(1):58-63
references.pmid: 19447202
references.citation: J Control Release. 2004 Nov 5;100(1):5-28
references.pmid: 15491807
references.citation: Acta Pharm. 2010 Dec;60(4):427-43
references.pmid: 21169135
references.citation: Pharm Res. 2006 Jul;23(7):1417-50
references.pmid: 16779701
references.citation: Drug Dev Ind Pharm. 2005 Jan;31(1):25-34
references.pmid: 15704855
references.citation: Adv Drug Deliv Rev. 2001 Aug 23;50(1-2):107-42
references.pmid: 11489336
references.citation: Pharm Res. 1997 Oct;14(10):1431-6
references.pmid: 9358557
references.citation: Colloids Surf B Biointerfaces. 2007 Oct 15;60(1):95-104
references.pmid: 17646089
references.citation: J Microencapsul. 2003 Jul-Aug;20(4):449-58
references.pmid: 12851045
references.citation: Drug Dev Ind Pharm. 2000 Oct;26(10):1085-90
references.pmid: 11028223
references.citation: J Pharm Pharm Sci. 2000 May-Aug;3(2):234-58
references.pmid: 10994037
references.citation: Eur J Pharm Biopharm. 2007 Jan;65(1):26-38
references.pmid: 16962750
references.citation: Adv Drug Deliv Rev. 2010 Jan 31;62(1):3-11
references.pmid: 19800377