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Related Concept Videos

Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

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...
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...
Factors Influencing Drug Absorption: Physicochemical Parameters01:22

Factors Influencing Drug Absorption: Physicochemical Parameters

The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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...
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: 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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Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
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Inorganic matrices: an answer to low drug solubility problem.

Luana Perioli1, Cinzia Pagano

  • 1Dipartimento di Chimica e Tecnologia del Farmaco, Università degli Studi di Perugia, Via del Liceo 1, Perugia 06123, Italy. luanaper@unipg.it

Expert Opinion on Drug Delivery
|October 16, 2012
PubMed
Summary

Improving drug delivery for poorly soluble active pharmaceutical ingredients (APIs) is crucial. Inorganic matrices offer a promising strategy to enhance the biopharmaceutical properties of these APIs without altering their chemical structure.

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Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier
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Dithranol as a Matrix for Matrix Assisted Laser Desorption/Ionization Imaging on a Fourier Transform Ion Cyclotron Resonance Mass Spectrometer
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Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier
10:16

Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier

Published on: February 8, 2017

Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Drug Delivery

Background:

  • Many active pharmaceutical ingredients (APIs) exhibit poor bioavailability due to low aqueous solubility and dissolution rates, particularly those in BCS classes II and IV.
  • This limitation often leads to inadequate therapeutic efficacy and necessitates higher doses, increasing the risk of adverse effects.
  • Dissolution rate is a key factor affecting the efficacy of orally administered drugs.

Purpose of the Study:

  • To review technological approaches for enhancing the solubility and dissolution rate of poorly soluble APIs.
  • To highlight the application of inorganic matrices as host materials for drug delivery.

Main Methods:

  • Review of common drug formulation strategies including nanocrystals, solid dispersions, cyclodextrins, and solid lipid nanoparticles.
  • Focus on inorganic matrices such as lamellar anionic clays and mesoporous materials as hosts for poorly soluble APIs.
  • Evaluation of host-guest composite systems for drug delivery.

Main Results:

  • Inorganic matrices provide a viable platform for creating host-guest composites.
  • These composites can significantly improve the biopharmaceutical properties of poorly soluble APIs.
  • The enhancement of drug properties is achievable without chemical modification of the API.

Conclusions:

  • Utilizing inorganic matrices for host-guest composite formation is an effective strategy for improving drug biopharmaceutical properties.
  • This approach offers a method to enhance the solubility and dissolution rate of challenging APIs.
  • The chemical integrity of the active pharmaceutical ingredient is maintained throughout the process.