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Related Concept Videos

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...
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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 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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Bioavailability refers to the extent and rate at which a drug reaches systemic circulation in its active form. Extent refers to the amount of the drug that makes it into circulation, while rate is the speed at which it enters circulation. It is influenced by several factors critical for optimizing drug formulations, dosing regimens, and therapeutic outcomes.Physicochemical properties of drugs and formulationsThe solubility, stability, and dissolution rate of a drug significantly impact its...
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,...
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Bioequivalence in generic drugs, such as tablets and capsules, refers to their pharmaceutical equivalence to the brand-name counterparts. However, for therapeutic equivalence, manufacturers must also consider physical attributes like size, shape, and weight (FDA Guidance for Industry, December 2003). Discrepancies in these aspects could impact patient compliance and cause medication errors. For instance, swallowing difficulties, often experienced with larger tablets or capsules, can lead to...

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Eudragit nanoparticles containing genistein: formulation, development, and bioavailability assessment.

Jingling Tang1, Na Xu, Hongyu Ji

  • 1Department of Pharmaceutics, School of Pharmacy, Harbin Medical University, Harbin, China.

International Journal of Nanomedicine
|November 11, 2011
PubMed
Summary
This summary is machine-generated.

Genistein nanoparticles significantly enhance oral bioavailability. This formulation improves the delivery of poorly water-soluble genistein, offering a promising approach for cancer chemoprevention and phytoestrogen applications.

Keywords:
bioavailabilitydissolutiongenisteinnanoparticlesnanoprecipitation technique

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Area of Science:

  • Pharmacology
  • Nanotechnology
  • Drug Delivery

Background:

  • Genistein, a key isoflavone, shows potential as a phytoestrogen and cancer chemoprevention agent.
  • Poor water solubility limits genistein's dissolution and oral bioavailability in conventional formulations.

Purpose of the Study:

  • To improve the oral bioavailability of genistein.
  • To develop genistein nanoparticles using Eudragit E100 via nanoprecipitation.

Main Methods:

  • Genistein nanoparticles were prepared using Eudragit E100 at a 1:10 mass ratio.
  • Nanoparticle characterization included particle size analysis (approx. 120 nm) and transmission electron microscopy (spherical shape).
  • Encapsulation efficiency and drug loading were determined.

Main Results:

  • Genistein nanoparticles exhibited approximately 50.61% encapsulation efficiency and 5.02% drug loading.
  • Drug release from nanoparticles was double that of conventional capsules.
  • Relative oral bioavailability of genistein nanoparticles in rats was 241.8% compared to suspension.

Conclusions:

  • Nanoparticle systems offer a promising strategy for enhancing the oral delivery of poorly water-soluble drugs.
  • This approach holds potential for improving the efficacy of genistein in therapeutic applications.
  • The developed genistein nanoparticles demonstrate superior bioavailability for oral administration.