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Published on: February 9, 2019
Solid lipid nanoparticles loaded with insulin by sodium cholate-phosphatidylcholine-based mixed micelles: preparation
Jie Liu1, Tao Gong, Changguang Wang
1Key Laboratory of Drug Targeting, Ministry of Education, Sichuan University, No. 17, Section 3, Southern Renmin Road, Chengdu, Sichuan 610041, PR China.
International Journal of Pharmaceutics
|April 13, 2007
Summary
This study presents a novel method for creating solid lipid nanoparticles (SLNs) loaded with insulin-mixed micelles (Ins-MMs), achieving high encapsulation efficiency and stability for protein drug delivery.
Area of Science:
- Nanotechnology
- Pharmaceutical Sciences
- Biomaterials
Background:
- Developing effective delivery systems for protein drugs like insulin is challenging due to stability and bioavailability issues.
- Solid lipid nanoparticles (SLNs) offer a promising platform for drug delivery, but optimizing their loading capacity for proteins requires advanced formulation strategies.
Purpose of the Study:
- To develop and optimize a novel reverse micelle-double emulsion method for preparing insulin-loaded solid lipid nanoparticles (Ins-MM-SLNs).
- To characterize the physical properties, encapsulation efficiency, and stability of the prepared Ins-MM-SLNs.
- To evaluate the drug release kinetics and confirm the integrity of insulin within the SLN formulation.
Main Methods:
- Preparation of insulin-mixed micelles (Ins-MMs) using sodium cholate (SC) and soybean phosphatidylcholine (SPC).
- Formulation of Ins-MM-SLNs using a novel reverse micelle-double emulsion method with stearic and palmitic acids.
- Characterization using photon correlation spectroscopy (PCS), transmission electron microscopy (TEM), scanning electron microscopy (SEM), high-performance liquid chromatography (HPLC), differential scanning calorimetry (DSC), fluorescence spectra, and polyacrylamide gel electrophoresis (PAGE).
Main Results:
- Optimized Ins-MM-SLNs exhibited a particle size of 114.7+/-4.68 nm and a zeta potential of -51.36+/-2.04 mV.
- High entrapment efficiency (97.78+/-0.37%) and drug loading capacity (18.92+/-0.07%) were achieved.
- TEM and SEM confirmed spherical nanostructures, DSC indicated no recrystallization, and PAGE confirmed insulin integrity.
- Drug release followed Weibull and Higuchi models, with good physical stability observed after 6 months at 4°C.
Conclusions:
- The novel reverse micelle-double emulsion method is effective for producing high-quality SLNs with excellent physical stability and high loading capacity for protein drugs like insulin.
- The prepared Ins-MM-SLNs demonstrate potential as a stable and efficient delivery system for protein therapeutics.
