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Related Concept Videos

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...
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 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,...
Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems01:22

Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems

Bioavailability is a critical pharmacological concept that measures the extent and rate at which an active drug ingredient or therapeutic moiety enters the systemic circulation, remaining unchanged. It's a pivotal factor in determining a drug's efficacy and safety.The Biopharmaceutics Classification System (BCS) plays an essential role in drug development by categorizing drugs into four classes based on their solubility and permeability. This classification aids in understanding drug absorption...
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...
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...

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Updated: Jun 21, 2026

PLGA Nanoparticles Formed by Single- or Double-emulsion with Vitamin E-TPGS
12:48

PLGA Nanoparticles Formed by Single- or Double-emulsion with Vitamin E-TPGS

Published on: December 27, 2013

Alpha-tocopherol-loaded Ca-pectinate microcapsules: optimization, in vitro release, and bioavailability.

Young-Bin Song1, Ji-Soo Lee, Hyeon Gyu Lee

  • 1Department of Food Nutrition, Hanyang University, Seongdong-gu, Seoul 133-791, Republic of Korea.

Colloids and Surfaces. B, Biointerfaces
|July 11, 2009
PubMed
Summary
This summary is machine-generated.

Optimized pectin-based microcapsules enhance alpha-tocopherol (TP) delivery. These microcapsules show sustained TP release in the intestine, improving oral bioavailability.

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Area of Science:

  • Food Science and Technology
  • Materials Science
  • Pharmaceutical Sciences

Background:

  • Alpha-tocopherol (TP), a vital nutrient, often faces challenges with oral bioavailability.
  • Microencapsulation is a promising technique to protect and control the release of active compounds like TP.

Purpose of the Study:

  • To optimize the preparation conditions for TP-loaded Ca-pectinate microcapsules using response surface methodology.
  • To evaluate the entrapment efficiency (EE) and in vitro/in vivo release characteristics of the optimized microcapsules.

Main Methods:

  • Response surface methodology was employed to determine optimal ratios of pectin:alpha-tocopherol, emulsifier concentration, and CaCl(2) concentration.
  • In vitro release studies were conducted in simulated gastric and intestinal fluids.
  • In vivo release studies were performed to assess the bioavailability of TP from the microcapsules.

Main Results:

  • Optimal microcapsule preparation involved a pectin:TP ratio of 9.7:6.3, 1.33% emulsifier, and 5.09% CaCl(2), achieving maximal entrapment efficiency.
  • The optimized microcapsules exhibited slow release in simulated gastric fluid and sustained release in simulated intestinal fluid.
  • In vivo studies confirmed the sustained release pattern and improved oral bioavailability of TP.

Conclusions:

  • Response surface methodology effectively optimized Ca-pectinate microcapsule formulation for maximal TP entrapment.
  • The developed microcapsules demonstrate potential for controlled and sustained oral delivery of alpha-tocopherol, enhancing its bioavailability.