Related Experiment Video
Updated: May 15, 2026
07:53
Encapsulation of Cancer Therapeutic Agent Dacarbazine Using Nanostructured Lipid Carrier
Published on: April 26, 2016
Formulation optimization and topical delivery of quercetin from solid lipid based nanosystems
Sonali Bose1, Yuechao Du, Paul Takhistov
1Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA.
International Journal of Pharmaceutics
|December 25, 2012
Summary
This study developed a stable, solvent-free nanosystem for topical quercetin delivery. The system effectively delivered quercetin into human skin, offering potential for enhanced protection against oxidative stress and UV damage.
Area of Science:
- Dermatology
- Nanotechnology
- Pharmacology
Background:
- Reactive oxygen species (ROS) cause oxidative stress, leading to skin damage through DNA breakage and enzyme inactivation.
- Quercetin, a potent flavonoid, exhibits high anti-radical activity, scavenges free radicals, and inhibits lipid peroxidation.
- Effective topical delivery of quercetin is crucial for mitigating UV-induced skin damage.
Purpose of the Study:
- To develop and evaluate a novel, solvent-free, solid lipid-based nanosystem for enhanced topical delivery of quercetin.
- To assess the physical stability, particle characteristics, and in vitro release profile of the quercetin-loaded nanosystem.
- To investigate the in vitro skin permeation and localization of quercetin delivered via the nanosystem.
Main Methods:
- Development of a solid lipid (glyceryl dibehenate) nanosystem using probe ultrasonication under solvent-free conditions.
- Evaluation of physical stability over 8 weeks at 2-8 °C and characterization using Transmission Electron Microscopy (TEM).
- In vitro release studies over 24 hours and in vitro permeation studies using full-thickness human skin.
Main Results:
- The optimized nanosystem exhibited good physical stability and spherical particles in the nanometer range (confirmed by TEM).
- In vitro release studies demonstrated a biphasic release pattern: an initial burst release followed by sustained release for 24 hours.
- In vitro permeation studies showed significantly higher quercetin localization within human skin compared to a micrometer-sized control formulation.
Conclusions:
- A stable, solvent-free solid lipid nanosystem for topical quercetin delivery has been successfully developed.
- The nanosystem facilitates enhanced quercetin permeation and accumulation in the epidermis, crucial for its protective effects against UV radiation.
- This formulation holds promise for improving the efficacy of quercetin in preventing UV-induced skin damage and cellular necrosis.
Related Concept Videos
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,...
01:24Modified-Release Drug Delivery Systems: Site-Targeted
Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
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...
01:23Oral Drug Delivery Systems: Introduction
Oral drug delivery is the most common route of administration due to its convenience, cost-effectiveness, and high patient compliance. It enables precise formulation to ensure proper drug dosage and bioavailability. The development of oral dosage forms considers drug properties such as solubility, stability, and absorption to optimize therapeutic efficacy.Tablets, capsules, liquids, and chewable formulations enhance drug stability, mask undesirable tastes, and improve patient experience.
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...
01:24Site-Targeted Drug Delivery Systems: Polymeric Carriers
Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...