Abstract
The objective of this work was to develop and characterize solid lipid nanoparticle (SLN)-loaded mucoadhesive films to reveal their potential as successful drug formulations. SLNs based on lipid (Lipoid S100) and surfactant (polysorbate 80) were prepared using the solvent-injection method, and their properties examined using experimental designs. Further, the marker coumarin 6 (C6) was solubilized in the particles as a model for a lipophilic drug. Lipid and surfactant concentrations influenced the particle size, while C6 had minor impact. The particle size distribution was narrow and the storage stability satisfactory for 4 months (4 ℃). The incorporation of the nanoparticles into a film matrix consisting of HPMC and glycerol, increased film thickness and flexibility, and slightly decreased the mechanical strength. The mucin interaction and disintegration time of the films were unimpaired. Film uniformity was satisfactory. Solubilisation in SLNs reduced the rate and extent of permeation of C6 through a monolayer of mucus-producing HT29-MTX cells. When the particles were incorporated into the mucoadhesive film, this effect was compensated for. In conclusion, this project was a first step in the successful development of an SLN-loaded mucoadhesive film formulation and served its purpose in revealing the formulation’s uniformity, mucoadhesiveness and biocompatibility.
Highlights
Water-soluble drugs pose a challenge for the formulation scientist
Solid lipid nanoparticles (SLNs) are lipid-based colloidal drug delivery systems consisting of a solid lipid core surrounded by one or more surfactants as stabilizing agents. (Geszke-Moritz and Moritz, 2016; Gordillo-Galeano and Mora-Huertas, 2018)
The apparent ad vantages of using SLNs above the more commonly employed polymeric nanoparticles is their superior ability to solubilize lipophilic drugs and great biocompatibility, especially when phospholipids are utilized (Geszke-Moritz and Moritz, 2016). The aim of this project was to lay the groundwork for the develop ment of an SLN-loaded mucoadhesive film formulation, which would allow the solubilisation of poorly water-soluble drugs, as well as provide taste masking; targeting the paediatric population
Summary
Amongst the many approaches to drug solubilisation, the use of lipid-based nanoparticles has emerged as an attractive one. Solid lipid nanoparticles (SLNs) are lipid-based colloidal drug delivery systems consisting of a solid lipid core surrounded by one or more surfactants as stabilizing agents. SLN are well-tolerated and able to solubi lize and protect drugs (Douroumis and Fahr, 2012; Geszke-Moritz and Moritz, 2016). SLNs are usually stable for over a year, when stored properly (Geszke-Moritz and Moritz, 2016). The formulation can be removed, if necessary Such a dosage form could be administered to unconscious patients as a less inva sive alternative to the usual parenteral routes of administration
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