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Related Concept Videos

Site-Targeted Drug Delivery Systems: Polymeric Carriers01:24

Site-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...
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

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...
Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability 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...
Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability 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,...
Bioplastics01:27

Bioplastics

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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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Published on: August 28, 2015

Issues in long-term protein delivery using biodegradable microparticles.

Mingli Ye1, Sungwon Kim, Kinam Park

  • 1Departments of Biomedical Engineering and Pharmaceutics, Purdue University, West Lafayette, Indiana 47907, USA.

Journal of Controlled Release : Official Journal of the Controlled Release Society
|May 25, 2010
PubMed
Summary
This summary is machine-generated.

Advances in biotechnology enable long-term protein drug delivery using biodegradable microparticles, primarily poly(lactic-co-glycolic acid) (PLGA). Optimizing formulation is key for controlled release and preserved bioactivity of protein therapeutics.

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Area of Science:

  • Biomaterials Science
  • Pharmaceutical Sciences
  • Drug Delivery

Background:

  • Biotechnology advances have increased the availability of bioactive protein drugs, necessitating the development of effective long-term delivery systems.
  • Biodegradable microparticulate systems, particularly those using poly(d,l-lactic-co-glycolic acid) (PLGA), are widely employed for controlled protein drug release over extended periods (days to months).
  • Established preparation methods include water/oil/water (W/O/W) double emulsion, solid/oil/water (S/O/W), water/oil/oil (W/O/O), spray drying, ultrasonic atomization, and electrospray.

Purpose of the Study:

  • To review critical factors in developing biodegradable microparticles for protein drug delivery, focusing on release profiles, particle characteristics, and protein integrity.
  • To categorize protein release profiles from microparticle formulations into four distinct types (A, B, C, D) based on burst release, release extent, and kinetics.
  • To highlight areas for improvement in drug loading efficiency, burst release control, and release kinetics for clinically successful long-term protein delivery systems.

Main Methods:

  • Review of existing literature on biodegradable microparticle preparation and protein drug delivery systems.
  • Analysis of protein release profiles, including burst release, duration, and extent.
  • Examination of factors influencing protein loading, encapsulation efficiency, and bioactivity preservation during processing and storage.

Main Results:

  • Protein loading in microparticles typically ranges from 0.5% to 20.0%, with an average of 6.7+/-4.6%.
  • Protein release profiles can be classified into four distinct categories (Types A, B, C, D) based on burst release magnitude and release kinetics.
  • Preserving the bioactivity of loaded protein drugs during formulation and storage is crucial, as demonstrated by studies using enzymes, insulin, erythropoietin, and growth factors.

Conclusions:

  • Development of clinically successful long-term protein delivery systems requires enhanced drug loading efficiency and precise control over initial burst release.
  • Controlling the protein release kinetics is essential for achieving predictable and effective therapeutic outcomes.
  • Further research should focus on optimizing formulations to ensure both efficient delivery and sustained bioactivity of protein therapeutics.