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Solid lipid nanoparticles loaded with insulin by sodium cholate-phosphatidylcholine-based mixed micelles: preparation and characterization.
Int J Pharm 2007; 340(1-2):153-62IJ

Abstract

Solid lipid nanoparticles (SLNs) loaded with insulin-mixed micelles (Ins-MMs) were prepared by a novel reverse micelle-double emulsion method, in which sodium cholate (SC) and soybean phosphatidylcholine (SPC) were employed to improve the liposolubility of insulin, and the mixture of stearic acid and palmitic acid were employed to prepare insulin loaded solid lipid nanoparticles (Ins-MM-SLNs). Some of the formulation parameters were optimized to obtain high quality nanoparticles. The particle size and zeta potential measured by photon correlation spectroscopy (PCS) were 114.7+/-4.68 nm and -51.36+/-2.04 mV, respectively. Nanospheres observed by transmission electron microscopy (TEM) and scanning electron microscopy (SEM) showed extremely spherical shape. The entrapment efficiency (EE%) and drug loading capacity (DL%) determined with high performance liquid chromatogram (HPLC) by modified ultracentrifuge method were 97.78+/-0.37% and 18.92+/-0.07%, respectively. Differential scanning calorimetry (DSC) of Ins-MM-SLNs indicated no tendency of recrystallisation. The core-shell drug loading pattern of the SLNs was confirmed by fluorescence spectra and polyacrylamide gel electrophoresis (PAGE) which also proved the integrity of insulin after being incorporated into lipid carrier. The drug release behavior was studied by in situ and externally sink method and the release pattern of drug was found to follow Weibull and Higuchi equations. Results of stability evaluation showed a relatively long-term stability after storage at 4 degrees C for 6 months. In conclusion, SLNs with small particle size, excellent physical stability, high entrapment efficiency, good loading capacity for protein drug can be produced by this novel reverse micelle-double emulsion method in present study.

Authors+Show Affiliations

Key Laboratory of Drug Targeting, Ministry of Education, Sichuan University, No. 17, Section 3, Southern Renmin Road, Chengdu, Sichuan 610041, PR China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

17428627

Citation

Liu, Jie, et al. "Solid Lipid Nanoparticles Loaded With Insulin By Sodium Cholate-phosphatidylcholine-based Mixed Micelles: Preparation and Characterization." International Journal of Pharmaceutics, vol. 340, no. 1-2, 2007, pp. 153-62.
Liu J, Gong T, Wang C, et al. Solid lipid nanoparticles loaded with insulin by sodium cholate-phosphatidylcholine-based mixed micelles: preparation and characterization. Int J Pharm. 2007;340(1-2):153-62.
Liu, J., Gong, T., Wang, C., Zhong, Z., & Zhang, Z. (2007). Solid lipid nanoparticles loaded with insulin by sodium cholate-phosphatidylcholine-based mixed micelles: preparation and characterization. International Journal of Pharmaceutics, 340(1-2), pp. 153-62.
Liu J, et al. Solid Lipid Nanoparticles Loaded With Insulin By Sodium Cholate-phosphatidylcholine-based Mixed Micelles: Preparation and Characterization. Int J Pharm. 2007 Aug 1;340(1-2):153-62. PubMed PMID: 17428627.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Solid lipid nanoparticles loaded with insulin by sodium cholate-phosphatidylcholine-based mixed micelles: preparation and characterization. AU - Liu,Jie, AU - Gong,Tao, AU - Wang,Changguang, AU - Zhong,Zhirong, AU - Zhang,Zhirong, Y1 - 2007/03/12/ PY - 2006/12/09/received PY - 2007/02/10/revised PY - 2007/03/07/accepted PY - 2007/4/13/pubmed PY - 2007/10/2/medline PY - 2007/4/13/entrez SP - 153 EP - 62 JF - International journal of pharmaceutics JO - Int J Pharm VL - 340 IS - 1-2 N2 - Solid lipid nanoparticles (SLNs) loaded with insulin-mixed micelles (Ins-MMs) were prepared by a novel reverse micelle-double emulsion method, in which sodium cholate (SC) and soybean phosphatidylcholine (SPC) were employed to improve the liposolubility of insulin, and the mixture of stearic acid and palmitic acid were employed to prepare insulin loaded solid lipid nanoparticles (Ins-MM-SLNs). Some of the formulation parameters were optimized to obtain high quality nanoparticles. The particle size and zeta potential measured by photon correlation spectroscopy (PCS) were 114.7+/-4.68 nm and -51.36+/-2.04 mV, respectively. Nanospheres observed by transmission electron microscopy (TEM) and scanning electron microscopy (SEM) showed extremely spherical shape. The entrapment efficiency (EE%) and drug loading capacity (DL%) determined with high performance liquid chromatogram (HPLC) by modified ultracentrifuge method were 97.78+/-0.37% and 18.92+/-0.07%, respectively. Differential scanning calorimetry (DSC) of Ins-MM-SLNs indicated no tendency of recrystallisation. The core-shell drug loading pattern of the SLNs was confirmed by fluorescence spectra and polyacrylamide gel electrophoresis (PAGE) which also proved the integrity of insulin after being incorporated into lipid carrier. The drug release behavior was studied by in situ and externally sink method and the release pattern of drug was found to follow Weibull and Higuchi equations. Results of stability evaluation showed a relatively long-term stability after storage at 4 degrees C for 6 months. In conclusion, SLNs with small particle size, excellent physical stability, high entrapment efficiency, good loading capacity for protein drug can be produced by this novel reverse micelle-double emulsion method in present study. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/17428627/Solid_lipid_nanoparticles_loaded_with_insulin_by_sodium_cholate_phosphatidylcholine_based_mixed_micelles:_preparation_and_characterization_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(07)00242-6 DB - PRIME DP - Unbound Medicine ER -