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Cyclosporine a loaded solid lipid nanoparticles: optimization of formulation, process variable and characterization.
Curr Drug Deliv 2008; 5(1):64-9CD

Abstract

Solid lipid nanoparticles (SLNs) loaded with Cyclosporine A using glyceryl monostearate (GMS) and glyceryl palmitostearate (GPS) as lipid matrices were prepared by melt-homogenization using high-pressure homogenizer. Various process parameters such as homogenization pressure, homogenization cycles and formulation parameters such as ratio of drug: lipid, emulsifier: lipid and emulsifier: co-emulsifier were optimized using particle size and entrapment efficiencies as the dependent variables. The mean particle size of optimized batches of the GMS SLN and GPS SLN were found to be 131 nm and 158 nm and their entrapment efficiencies were 83 +/- 3.08% and 97 +/- 2.59% respectively. To improve the handling processing and stability of the prepared SLNs, the SLN dispersions were spray dried and its effect on size and reconstitution parameters were evaluated. The spray drying of SLNs did not significantly alter the size of SLNs and they exhibited good redispersibility. Solid state studies such as Infra Red Spectroscopy and Differential Scanning Calorimetry indicated absence of any chemical interaction between Cyclosporine A and the lipids. Scanning Electron Microscopy of optimized formulations showed spherical shape with smooth and non porous surface. In vitro release studies revealed that GMS based SLNs released the drug faster (41.12% in 20 hours) than GPS SLNs (7.958% in 20 hours). Release of Cyclosporine A from GMS SLN followed Higuchi equation better than first order while release from GPS SLN followed first order better than Higuchi model.

Authors+Show Affiliations

Pharmacy Department, Faculty of Technology & Engineering, The Maharaja Sayajirao University of Baroda, Kalabhavan, Vadodara, Gujarat, India.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

18220553

Citation

Varia, Jigisha K., et al. "Cyclosporine a Loaded Solid Lipid Nanoparticles: Optimization of Formulation, Process Variable and Characterization." Current Drug Delivery, vol. 5, no. 1, 2008, pp. 64-9.
Varia JK, Dodiya SS, Sawant KK. Cyclosporine a loaded solid lipid nanoparticles: optimization of formulation, process variable and characterization. Curr Drug Deliv. 2008;5(1):64-9.
Varia, J. K., Dodiya, S. S., & Sawant, K. K. (2008). Cyclosporine a loaded solid lipid nanoparticles: optimization of formulation, process variable and characterization. Current Drug Delivery, 5(1), pp. 64-9.
Varia JK, Dodiya SS, Sawant KK. Cyclosporine a Loaded Solid Lipid Nanoparticles: Optimization of Formulation, Process Variable and Characterization. Curr Drug Deliv. 2008;5(1):64-9. PubMed PMID: 18220553.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Cyclosporine a loaded solid lipid nanoparticles: optimization of formulation, process variable and characterization. AU - Varia,Jigisha K, AU - Dodiya,Shamsunder S, AU - Sawant,Krutika K, PY - 2008/1/29/pubmed PY - 2008/3/1/medline PY - 2008/1/29/entrez SP - 64 EP - 9 JF - Current drug delivery JO - Curr Drug Deliv VL - 5 IS - 1 N2 - Solid lipid nanoparticles (SLNs) loaded with Cyclosporine A using glyceryl monostearate (GMS) and glyceryl palmitostearate (GPS) as lipid matrices were prepared by melt-homogenization using high-pressure homogenizer. Various process parameters such as homogenization pressure, homogenization cycles and formulation parameters such as ratio of drug: lipid, emulsifier: lipid and emulsifier: co-emulsifier were optimized using particle size and entrapment efficiencies as the dependent variables. The mean particle size of optimized batches of the GMS SLN and GPS SLN were found to be 131 nm and 158 nm and their entrapment efficiencies were 83 +/- 3.08% and 97 +/- 2.59% respectively. To improve the handling processing and stability of the prepared SLNs, the SLN dispersions were spray dried and its effect on size and reconstitution parameters were evaluated. The spray drying of SLNs did not significantly alter the size of SLNs and they exhibited good redispersibility. Solid state studies such as Infra Red Spectroscopy and Differential Scanning Calorimetry indicated absence of any chemical interaction between Cyclosporine A and the lipids. Scanning Electron Microscopy of optimized formulations showed spherical shape with smooth and non porous surface. In vitro release studies revealed that GMS based SLNs released the drug faster (41.12% in 20 hours) than GPS SLNs (7.958% in 20 hours). Release of Cyclosporine A from GMS SLN followed Higuchi equation better than first order while release from GPS SLN followed first order better than Higuchi model. SN - 1567-2018 UR - https://www.unboundmedicine.com/medline/citation/18220553/Cyclosporine_a_loaded_solid_lipid_nanoparticles:_optimization_of_formulation_process_variable_and_characterization_ L2 - http://www.eurekaselect.com/66185/article DB - PRIME DP - Unbound Medicine ER -