Related Experiment Video
Updated: Jun 19, 2026
09:34
Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells
Published on: February 9, 2019
Corticosteroid solubility and lipid polarity control release from solid lipid nanoparticles.
Louise B Jensen1, Emily Magnussson, Linda Gunnarsson
1LEO Pharma A/S, Industriparken 55, DK-2750 Ballerup, Denmark. louise.bastholm-jensen@leo-pharma.com
International Journal of Pharmaceutics
|October 20, 2009
Summary
Solid lipid nanoparticles (SLN) offer controlled drug release for skin. Drug solubility and lipid composition significantly impact corticosteroid release from SLN, optimizing topical delivery.
Area of Science:
- Pharmaceutical Sciences
- Nanotechnology
- Dermatology
Background:
- Solid lipid nanoparticles (SLN) are a promising drug delivery system for topical administration.
- Their solid matrix allows for efficient drug encapsulation and controlled release.
- Understanding factors influencing drug release is crucial for optimizing SLN formulations.
Purpose of the Study:
- To investigate the impact of lipid composition and drug lipophilicity on corticosteroid release from SLN.
- To determine how variations in monoglyceride content and fatty acid chain length affect drug release.
- To assess the influence of corticosteroid physicochemical properties on in vitro release profiles.
Main Methods:
- Formulation of SLN with varying lipid compositions (monoglyceride content, fatty acid chain length).
- In vitro release studies of betamethasone-17-valerate (BMV) and other corticosteroid derivatives.
- Analysis of drug release kinetics in relation to drug lipophilicity and lipid phase partitioning.
Main Results:
- Increased monoglyceride content in SLN enhanced the release of betamethasone-17-valerate.
- Corticosteroid release rate was directly influenced by drug substance lipophilicity.
- Release profiles indicated drug partitioning to the aqueous phase, consistent with zero-order kinetics.
Conclusions:
- Corticosteroid solubility within the lipid phase is a key determinant of drug distribution and release from SLN.
- Drug partitioning behavior and lipid polarity are critical parameters for optimizing SLN release characteristics.
- Knowledge of drug-lipid interactions is essential for designing effective topical corticosteroid delivery systems using SLN.
Related Concept Videos
01:21Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles in drug...
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles in drug...
01:16Bioavailability Enhancement: Drug Solubility Enhancement
Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are employed to...
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
01:27Bioavailability Enhancement: Drug Permeability Enhancement
After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...
01:20Modified-Release Drug Delivery Systems: Influencing Factors
Modified-release drug delivery systems are designed to optimize the therapeutic effect of drugs by minimizing side effects, reducing the dosage required, and controlling drug release to align with pharmacokinetic and pharmacodynamic needs. The system depends on two key factors: the drug's release from the formulation and its movement through the body to the target site. Unlike conventional dosage forms, where absorption is the limiting step, the rate of drug release is the key determinant in...