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Modified-Release Drug Delivery Systems: Rate-Programmed II01:19

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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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...
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Modified-release drug delivery systems improve drug efficacy and minimize side effects by controlling the rate and location of drug release. These systems fall into three categories: rate-programmed, stimuli-activated, and site-targeted.Rate-programmed systems release drugs at a predetermined rate, maintaining consistent therapeutic levels and reducing fluctuations that could lead to toxicity or subtherapeutic effects. These systems use polymeric matrices, reservoir-based designs, or osmotic...
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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...
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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
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Using a drug to structure its release matrix and release profile.

Michael A Brook1, Alison C Holloway, Kenneth K Ng

  • 1Department of Chemistry, McMaster University, 1280 Main Street West, Hamilton, Ontario, Canada. mabrook@mcmaster.ca

International Journal of Pharmaceutics
|April 15, 2008
PubMed
Summary

Linoleic acid modifies silicone elastomer morphology, improving controlled release of hydrophilic drugs. This innovation enhances drug delivery systems by preventing burst release and enabling longer-term therapeutic effects.

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Area of Science:

  • Biomaterials Science
  • Drug Delivery Systems
  • Polymer Chemistry

Background:

  • Silicone elastomers are effective matrices for hydrophobic drug delivery.
  • Controlled release of hydrophilic drugs from silicone elastomers remains challenging, often resulting in burst release profiles, even with polar excipients like poly(ethylene oxide) (PEO).

Purpose of the Study:

  • To investigate the effect of linoleic acid on the morphology of silicone+PEO elastomers.
  • To determine if linoleic acid can improve the controlled release of hydrophilic drugs from these elastomers.
  • To examine the relationship between excipients, silicone morphology, and drug release profiles.

Main Methods:

  • Incorporation of linoleic acid into silicone precursors containing PEO and a model hydrophilic drug (nicotine).
  • Fabrication of silicone+PEO elastomers with varying linoleic acid concentrations.
  • In vitro drug release studies to assess release kinetics.
  • Morphological analysis of the elastomer matrices.

Main Results:

  • Linoleic acid altered the internal morphology of the silicone+PEO elastomers.
  • This morphological change led to a modified distribution of hydrophilic PEO/drug domains within the silicone matrix.
  • The modified elastomers demonstrated controlled in vitro release of the hydrophilic drug, mitigating burst release.

Conclusions:

  • Linoleic acid acts as a morphology-modifying excipient in silicone elastomers.
  • This modification enables controlled release of hydrophilic drugs, overcoming previous limitations.
  • The findings offer a new strategy for developing advanced silicone-based drug delivery systems for hydrophilic compounds.