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Formulation, optimization, and characterization of rifampicin-loaded solid lipid nanoparticles for the treatment of tuberculosis.
Drug Dev Ind Pharm 2018; 44(12):1975-1989DD

Abstract

Mycobacterium tuberculosis, being the causative infectious agent, is the leading cause of death worldwide amongst the infectious disease. The low bioavailability of rifampicin (RIF), one of the vital constituent of antitubercular therapy, instigates an urge to develop nanocarrier, which can prevent its degradation in the acidic pH of the stomach. Solid lipid nanoparticles (SLNs) have been proven to be promising versatile platform for oral delivery of lipophilic drugs. Therefore, the current investigation demonstrates development of RIF-loaded solid lipid nanoparticles (RIF-SLNs) using high-pressure homogenization technique by employing a three-level, three-factor Box-Behnken design. Concentration of drug, concentration of emulsifier, and homogenization pressure were selected as an independent variables, and %drug loading (%DL), %entrapment efficiency (%EE), and particle size were selected as dependent variables. The developed RIF-SLNs were characterized for particle size, polydispersity index, zeta potential, %EE, %DL, differential scanning calorimetry, X-ray diffraction, and TEM analysis. The mean diameter of RIF-SLNs was found to be 456 ± 11 nm, %EE of 84.12 ± 2.78%, and %DL of 15.68 ± 1.52%. The in vitro lipolysis experiments revealed that RIF-SLNs stabilized using poloxamer 188, exhibited antilipolytic effect. Furthermore, the in vitro GI stability studies (at pH 1.2, pH 4.5, pH 6.8, and pH 7.4) revealed that the developed system could withstand various gastrointestinal tract media. The in vitro dissolution studies depicted biphasic drug release profile for drug-loaded SLNs revealing best fit with Weibull model. The accelerated stability studies for 6 months does not revealed any significant change in characteristics of developed RIF-SLNs.

Authors+Show Affiliations

a Department of Pharmaceutics , Institute of Pharmacy, Nirma University, SG Highway, Chharodi , Ahmedabad , Gujarat , India.a Department of Pharmaceutics , Institute of Pharmacy, Nirma University, SG Highway, Chharodi , Ahmedabad , Gujarat , India.a Department of Pharmaceutics , Institute of Pharmacy, Nirma University, SG Highway, Chharodi , Ahmedabad , Gujarat , India.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30058392

Citation

Chokshi, Nimitt V., et al. "Formulation, Optimization, and Characterization of Rifampicin-loaded Solid Lipid Nanoparticles for the Treatment of Tuberculosis." Drug Development and Industrial Pharmacy, vol. 44, no. 12, 2018, pp. 1975-1989.
Chokshi NV, Khatri HN, Patel MM. Formulation, optimization, and characterization of rifampicin-loaded solid lipid nanoparticles for the treatment of tuberculosis. Drug Dev Ind Pharm. 2018;44(12):1975-1989.
Chokshi, N. V., Khatri, H. N., & Patel, M. M. (2018). Formulation, optimization, and characterization of rifampicin-loaded solid lipid nanoparticles for the treatment of tuberculosis. Drug Development and Industrial Pharmacy, 44(12), pp. 1975-1989. doi:10.1080/03639045.2018.1506472.
Chokshi NV, Khatri HN, Patel MM. Formulation, Optimization, and Characterization of Rifampicin-loaded Solid Lipid Nanoparticles for the Treatment of Tuberculosis. Drug Dev Ind Pharm. 2018;44(12):1975-1989. PubMed PMID: 30058392.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation, optimization, and characterization of rifampicin-loaded solid lipid nanoparticles for the treatment of tuberculosis. AU - Chokshi,Nimitt V, AU - Khatri,Hiren N, AU - Patel,Mayur M, Y1 - 2018/08/31/ PY - 2018/7/31/pubmed PY - 2018/7/31/medline PY - 2018/7/31/entrez KW - Box–Behnken design KW - drug release kinetics KW - lipid nanoparticles KW - lipolysis model KW - long chain lipids KW - lymphatic delivery SP - 1975 EP - 1989 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 44 IS - 12 N2 - Mycobacterium tuberculosis, being the causative infectious agent, is the leading cause of death worldwide amongst the infectious disease. The low bioavailability of rifampicin (RIF), one of the vital constituent of antitubercular therapy, instigates an urge to develop nanocarrier, which can prevent its degradation in the acidic pH of the stomach. Solid lipid nanoparticles (SLNs) have been proven to be promising versatile platform for oral delivery of lipophilic drugs. Therefore, the current investigation demonstrates development of RIF-loaded solid lipid nanoparticles (RIF-SLNs) using high-pressure homogenization technique by employing a three-level, three-factor Box-Behnken design. Concentration of drug, concentration of emulsifier, and homogenization pressure were selected as an independent variables, and %drug loading (%DL), %entrapment efficiency (%EE), and particle size were selected as dependent variables. The developed RIF-SLNs were characterized for particle size, polydispersity index, zeta potential, %EE, %DL, differential scanning calorimetry, X-ray diffraction, and TEM analysis. The mean diameter of RIF-SLNs was found to be 456 ± 11 nm, %EE of 84.12 ± 2.78%, and %DL of 15.68 ± 1.52%. The in vitro lipolysis experiments revealed that RIF-SLNs stabilized using poloxamer 188, exhibited antilipolytic effect. Furthermore, the in vitro GI stability studies (at pH 1.2, pH 4.5, pH 6.8, and pH 7.4) revealed that the developed system could withstand various gastrointestinal tract media. The in vitro dissolution studies depicted biphasic drug release profile for drug-loaded SLNs revealing best fit with Weibull model. The accelerated stability studies for 6 months does not revealed any significant change in characteristics of developed RIF-SLNs. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/30058392/Formulation_optimization_and_characterization_of_rifampicin_loaded_solid_lipid_nanoparticles_for_the_treatment_of_tuberculosis_ L2 - http://www.tandfonline.com/doi/full/10.1080/03639045.2018.1506472 DB - PRIME DP - Unbound Medicine ER -