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Bioavailability Enhancement: Drug Solubility Enhancement01:16

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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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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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Factors Influencing Drug Absorption: Drug Dissolution01:27

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The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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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...
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Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
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Curcumin-Eudragit® E PO solid dispersion: A simple and potent method to solve the problems of curcumin.

Jinglei Li1, Il Woo Lee1, Gye Hwa Shin1

  • 1School of Life Sciences and Biotechnology, Korea University, 5-Ka, Anam-Dong, Sungbuk-Ku, Seoul 136-701, Republic of Korea.

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V
|June 16, 2015
PubMed
Summary

This study developed a curcumin-Eudragit® E PO solid dispersion (Cur@EPO) enhancing curcumin

Keywords:
Acetone (PubChem CID: 180)CurcuminCurcumin (PubChem CID: 969516)Eudragit® E POEudragit® E PO (PubChem CID: 107676)Sodium Acetate (PubChem CID: 517045)Solid dispersionStabilityTransdermal administrationWater solubility

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Area of Science:

  • Pharmaceutical Technology
  • Materials Science

Background:

  • Curcumin exhibits poor water solubility, limiting its therapeutic applications.
  • Developing effective delivery systems is crucial for enhancing curcumin's bioavailability and efficacy.

Purpose of the Study:

  • To create a solid dispersion of curcumin in Eudragit® E PO (Cur@EPO) to improve its solubility and explore its potential for transdermal delivery.
  • To characterize the solid dispersion and investigate curcumin's release profile and stability.

Main Methods:

  • Simple solution mixing method for creating the solid dispersion.
  • Fourier transform infrared spectroscopy (FTIR) and (1)H Nuclear Magnetic Resonance (NMR) for interaction analysis.
  • pH challenge, UV irradiation, and in vitro transdermal tests for stability and release studies.

Main Results:

  • Curcumin was successfully dispersed in the amorphous state within the Eudragit® E PO matrix, significantly increasing water solubility.
  • Hydrogen bonding was observed between curcumin's hydroxyl group and the polymer's carbonyl group.
  • Cur@EPO demonstrated protective effects against pH changes and UV irradiation, showing sustained curcumin release influenced by pH.
  • In vitro transdermal studies indicated potential for Cur@EPO as a transdermal delivery vehicle.

Conclusions:

  • Curcumin-Eudragit® E PO solid dispersion (Cur@EPO) effectively enhances curcumin's solubility and stability.
  • The developed system shows promise for sustained release and potential transdermal delivery of curcumin.