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Related Concept Videos

Modified-Release Drug Delivery Systems: Influencing Factors01:20

Modified-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...
Modified-Release Drug Delivery Systems: Drug Release Characteristics01:22

Modified-Release Drug Delivery Systems: Drug Release Characteristics

Drug release from modified-release dosage forms is designed to achieve specific therapeutic effects by controlling the rate and extent of drug release. The classification of these drug release systems is based on key pharmacokinetic assumptions: drug disposition follows first-order kinetics, drug release is the rate-limiting step in absorption, and the released drug is rapidly and completely absorbed.There are four major models of drug release patterns. The first model is the slow zero-order...
Oral Drug Delivery Systems: Delayed-Release Systems01:11

Oral 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...
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Rate-programmed drug delivery systems (DDS) are designed to release drugs at specific, controlled rates to maintain consistent therapeutic levels. These systems are categorized based on their release mechanisms, including dissolution-controlled DDS, diffusion-controlled DDS, and combined dissolution-diffusion-controlled DDS.In dissolution-controlled DDS, the release rate depends on the slow dissolution of the drug itself or the surrounding matrix. Drugs with inherently slow dissolution rates,...
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Bioavailability 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...
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Modified-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...

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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
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New solid lipid microparticles for controlled ibuprofen release: formulation and characterization study.

Laurent Perge1, Mike Robitzer, Coralie Guillemot

  • 1Institut Charles Gerhardt Montpellier UMR 5253 CNRS-UM2-ENSCM-UM1, Matériaux Avancés pour Catalyse et Santé, ENSCM, 8 rue de l'Ecole Normale, 34296 Montpellier Cedex 5, France.

International Journal of Pharmaceutics
|October 27, 2011
PubMed
Summary

Researchers developed sustained-release ibuprofen microparticles using cetyl alcohol and silica nanoparticles. Hydrophobic silica improved microparticle homogeneity and influenced drug release kinetics by affecting particle size.

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Area of Science:

  • Materials Science
  • Pharmaceutical Technology
  • Nanotechnology

Background:

  • Developing sustained-release drug delivery systems is crucial for improving therapeutic efficacy and patient compliance.
  • Solid lipid microparticles offer a promising platform for drug encapsulation due to their biocompatibility and controlled release properties.
  • The incorporation of nanoparticles can modify the physicochemical properties and drug release profiles of microparticulate systems.

Purpose of the Study:

  • To prepare novel sustained-release ibuprofen composite microparticles using a hot melt dispersion method.
  • To investigate the effect of colloidal silicon dioxide nanoparticles (Aerosil 200 and Aerosil R974) on the characteristics and drug release kinetics of ibuprofen-loaded solid lipid microparticles.
  • To explore the influence of nanoparticle type and dispersion method on the internal structure and homogeneity of the microparticles.

Main Methods:

  • Hot melt dispersion technique was employed to prepare ibuprofen-loaded cetyl alcohol microparticles.
  • Colloidal silicon dioxide nanoparticles (hydrophilic Aerosil 200, hydrophobic Aerosil R974) were dispersed in either the oily or aqueous phase.
  • Scanning electron microscopy with a silicon probe was used for structural analysis and elemental mapping.
  • Drug release kinetics were evaluated to assess the impact of nanoparticle incorporation.

Main Results:

  • Large, surfactant-free, free-flowing microparticles (approx. 400 μm diameter) were successfully prepared.
  • Silicon was localized in the oily core of all composite microparticles, irrespective of silica type or dispersion method.
  • The nature of silica nanoparticles and their dispersion method influenced internal structure and nanoparticle aggregation.
  • Hydrophobic Aerosil R974 resulted in more homogeneous microparticle formation.
  • Silica nanoparticles did not alter the thermal properties or crystalline state of ibuprofen and cetyl alcohol.
  • Drug release kinetics were affected by nanoparticle incorporation, primarily due to changes in microparticle size.

Conclusions:

  • Sustained-release ibuprofen composite microparticles can be effectively prepared using hot melt dispersion with cetyl alcohol and silica nanoparticles.
  • The choice of silica nanoparticle (hydrophilic vs. hydrophobic) and dispersion strategy significantly impacts microparticle morphology and internal structure.
  • Hydrophobic silica nanoparticles promote homogeneity, while particle size increase, influenced by silica, is a key factor modulating drug release rates.
  • This study highlights the potential of tailored nanoparticle incorporation for controlling drug release from solid lipid microparticles.