Systematic Procedures for Formulation Design of Drug-Loaded Solid Lipid Microparticles: Selection of Carrier Material and Stabilizer

Abstract

A systematic procedure is presented for selecting the carrier material and stabilizer for drug-loaded solid lipid microparticles (SLMs). Heuristics criteria as well as investigation methods are proposed. The proposed procedure is based on the summaries of the authors' investigation and the accumulated heuristics derived from the available literature works. The physical properties of carrier materials, drug distribution in the carrier matrix, the compatibility between drugs and carrier materials, and the crystal structures of carrier matrices are taken into account in the selection of the carrier materials. In stabilizer selection, the coverage of stabilizer molecules on particle surfaces and the electrostatic repulsion and steric repulsion of stabilizers should be considered. The presented heuristics and criteria are to assist with decision making in new SLM development. This is demonstrated with an application case, in which a clozapine-loaded SLM formulation is designed, to illustrate the selection of carrier materials and stabilizers. Experiments and testing have confirmed the effectiveness of the proposed procedure and heuristics.

Formulation, characterization and pulmonary deposition of nebulized celecoxib encapsulated nanostructured lipid carriers

“…Similar observations were made by Zhang et al [29] where solid lipid microparticles prepared with Compritol showed slower clozapine release compared to microparticles made with tristearin mainly because of the distribution of clozapine in the inner area of the lipid matrix and has longer diffusion path length.…”

Translocation of cell penetrating peptide engrafted nanoparticles across skin layers

“…Cxb has initiate the diffusion from Miglyol oil phase to the solid outer surface of the nanoparticles before undergoing partitioning between outer lipid and the bulk aqueous phase. Similar observations were made by Zhang et al [27] where solid lipid microparticles prepared with Compritol showed slower clozapine release comparing with microparticles made with tristearin mainly because of the distribution of clozapine in the inner area of the lipid matrix and longer diffusion path length.…”

Improved and Safe Transcorneal Delivery of Flurbiprofen by NLC and NLC-Based Hydrogels

“…The mono-and diglycerides of glyceryl behenate possess surface active properties (Hydrophilic-Lipophilic Balance (HLB) = 2-5). 28 The use of C888 facilitates the emulsification process by forming surfactant films more rapidly, and thus prevents particle aggregation during a certain period of time. Replacing more than 30% of solid lipid by oil, the percentage of mono-and diacylglycerols was reduced significatively.…”