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Related Concept Videos

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...
Modified-Release Drug Delivery Systems: Rate-Programmed I01:22

Modified-Release Drug Delivery Systems: Rate-Programmed I

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,...
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...
Modified-Release Drug Delivery Systems: Bioavailability01:30

Modified-Release Drug Delivery Systems: Bioavailability

Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...
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...
Modified-Release Drug Delivery Systems: Classification01:23

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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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PLGA Nanoparticles Formed by Single- or Double-emulsion with Vitamin E-TPGS
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Published on: December 27, 2013

Quantifying drug release from PLGA nanoparticulates.

Owen I Corrigan1, Xue Li

  • 1School of Pharmacy and Pharmaceutical Sciences, University of Dublin, Trinity College, Dublin, Ireland. ocorrign@tcd.ie

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
|April 22, 2009
PubMed
Summary

This study reveals drug release from PLGA nanoparticulates involves diffusion and polymer degradation. Higher drug loading and solubility increase initial burst release, impacting release kinetics.

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Area of Science:

  • Materials Science
  • Pharmaceutical Sciences
  • Polymer Chemistry

Background:

  • Poly(lactic-co-glycolic acid) (PLGA) nanoparticulates are widely used for drug delivery.
  • Understanding drug release mechanisms is crucial for optimizing therapeutic efficacy.

Purpose of the Study:

  • To investigate the release mechanisms of small molecules and macromolecules from PLGA nanoparticulates.
  • To elucidate the influence of drug properties and loading on release kinetics.

Main Methods:

  • Preparation of PLGA (50:50) nanoparticulates (400-700nm) with <10% drug loading using emulsification/solvent evaporation.
  • In vitro release studies in phosphate buffer (pH 7.4, 37°C) for various active pharmaceutical ingredients (APIs).

Main Results:

  • Release profiles showed an initial burst, followed by a lag phase, and then an accelerated release phase.
  • The initial burst release correlated with API loading and solubility.
  • Polymer degradation significantly influenced the later phase of API release, with acidic hydrophobic drugs having a greater impact than hydrophilic proteins.

Conclusions:

  • Drug release from PLGA nanoparticulates is a dual mechanism involving diffusion and polymer erosion.
  • API physicochemical properties and loading influence release kinetics, particularly the burst release.
  • PLGA nanoparticulates demonstrate tunable release profiles dependent on drug characteristics and degradation.