Related Experiment Video
Updated: May 28, 2026
09:34
Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells
Published on: February 9, 2019
Layered lipid microcapsules for mesalazine delayed-release in children
Anna Giulia Balducci1, Gaia Colombo, Giuseppe Corace
1Department of Pharmacy, University of Parma, Viale G.P. Usberti 27/A, 43124 Parma, Italy.
International Journal of Pharmaceutics
|October 18, 2011
Summary
New mesalazine microcapsules offer a delayed-release dosage form dispersible in water. This formulation facilitates swallowing for adults and children, ensuring pH-dependent drug release for effective oral use.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Materials Science
Background:
- Mesalazine is a key treatment for inflammatory bowel disease.
- Swallowing solid dosage forms can be challenging for pediatric and adult patients.
- Developing water-dispersible, delayed-release formulations is crucial for patient compliance.
Purpose of the Study:
- To develop a novel, water-dispersible, delayed-release mesalazine dosage form.
- To create a formulation suitable for extemporaneous oral administration in adults and children.
- To achieve pH-dependent drug release characteristics.
Main Methods:
- Mesalazine microparticles were prepared using spray-congealing with carnauba wax.
- Mesalazine lipid microcapsules with embedded carnauba wax cores were formed via a second spray-congealing step.
- Microcapsules were dry-coated with mannitol/lecithin microparticles using spray-drying to enhance water dispersibility and achieve pH-dependence.
Main Results:
- The developed mesalazine lipid microcapsules exhibited a reservoir structure with embedded carnauba wax cores.
- Dry coating with mannitol/lecithin improved water dispersion properties.
- Release studies demonstrated delayed-release behavior, with <10% mesalazine release in acidic conditions and complete release (>90%) in phosphate buffer (pH 7.4) within 4-5 hours.
Conclusions:
- Layering with hydrophilic excipient microparticles successfully created a pH-dependent dosage form.
- The developed formulation is suitable for extemporaneous oral use, addressing swallowing difficulties.
- This novel dosage form enhances mesalazine delivery for patients requiring delayed and targeted release.
Related Concept Videos
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...
01:26Oral Drug Delivery Systems: Continuous-Release Systems
Continuous-release drug delivery systems offer a strategic approach to maintaining therapeutic drug levels over extended periods following oral administration. By modulating the release rate of active pharmaceutical ingredients, these systems minimize fluctuations in plasma concentrations, which enhances clinical efficacy and reduces the need for frequent dosing. Such characteristics make them particularly advantageous in managing chronic diseases where patient adherence and stable drug...
01:29Drugs for Treatment of Ulcerative Colitis in IBD
Ulcerative colitis is a chronic inflammatory condition primarily affecting the colon and rectum. The primary drugs used in the treatment of ulcerative colitis are aminosalicylates. They exhibit anti-inflammatory and immunosuppressive properties. They modulate inflammatory mediators and inhibit the activity of nuclear factor κB (NF-κB). Aminosalicylates also reduce inflammation by inhibiting prostaglandin and leukotriene production and decreasing neutrophil chemotaxis and superoxide generation.
01:19Modified-Release Drug Delivery Systems: Rate-Programmed II
Rate-programmed drug delivery systems release drugs in a controlled manner to maintain therapeutic levels. Three main designs include reservoir, matrix, and hybrid systems.Reservoir systems consist of a drug core enclosed within a membrane that controls drug release. In non-swelling reservoir systems, polymers like ethyl cellulose or polymethacrylates are used. These do not hydrate in aqueous media and control release through membrane thickness, porosity, or insolubility. This type includes...
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,...
01:05Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...