Related Experiment Video
Updated: Aug 14, 2026
08:18
Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
Published on: July 27, 2022
Design, development and optimization of nimesulide-loaded liposomal systems for topical application
Bhupinder Singh1, Gaurav Mehta, Rajiv Kumar
1University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India. bsbhoop@yahoo.com
Current Drug Delivery
|November 25, 2005
Summary
Liposomes enhanced topical delivery of nimesulide, a non-steroidal anti-inflammatory drug. This formulation showed improved skin retention and superior anti-inflammatory effects compared to conventional gels.
Area of Science:
- Pharmaceutics
- Drug Delivery Systems
- Nanotechnology
Background:
- Topical administration of non-steroidal anti-inflammatory drugs (NSAIDs) like nimesulide often faces challenges with efficacy and skin penetration.
- Liposomes offer a promising drug delivery system to enhance the performance of topical medications.
Purpose of the Study:
- To develop and optimize multilamellar liposomes for improved topical delivery of nimesulide.
- To evaluate the anti-inflammatory efficacy and skin permeation characteristics of nimesulide-loaded liposomes.
Main Methods:
- Nimesulide was incorporated into multilamellar liposomes using the thin film hydration technique.
- Liposomal formulations were characterized for drug entrapment, vesicular properties, and drug release.
- Optimization was performed using a 3(2) factorial design.
- Drug permeation, retention, and anti-inflammatory activity were assessed using ex vivo skin models and an in vivo rat paw edema model.
Main Results:
- Optimized liposomes demonstrated desirable vesicular properties and efficient drug entrapment.
- Liposomal nimesulide exhibited significantly higher skin retention compared to a simple methanolic solution.
- The liposomal formulation showed superior anti-inflammatory activity in the carrageenan-induced rat paw edema model compared to marketed and Carbopol gel formulations.
Conclusions:
- Multilamellar liposomes are an effective strategy for enhancing the topical delivery of nimesulide.
- Liposomal nimesulide offers improved anti-inflammatory efficacy and better skin retention for topical applications.
Related Concept Videos
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.
01:27Bioavailability 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,...
01:24Site-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...
01:11Oral Drug Delivery Systems: Delayed-Release Systems
Delayed-release drug delivery systems are specialized pharmaceutical formulations designed to postpone the release of active compounds until the drug reaches a specific region of the gastrointestinal (GI) tract, typically the intestine. These systems are essential for drugs that may cause gastric irritation, are unstable in acidic environments, or need to exert therapeutic effects locally in the intestinal or colonic regions.The core feature of delayed-release systems is the use of enteric...
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...
01:16Bioavailability 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...