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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,...
Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

Factors Affecting Dissolution: Particle Size and Effective Surface Area

Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are employed to...
Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
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...
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...

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Related Experiment Video

Updated: May 27, 2026

Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells
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Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells

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Fast dissolving β-lapachone particles and tablets: an approach using surface adsorption technique.

Marcílio S S Cunha-Filho1, Ramón Martínez-Pacheco, Mariana Landin

  • 1Instituto de Ciências da Saúde, Campus Universitário de Sinop, Universidade Federal de Mato Grosso-UFMT, Avenida Alexandre Ferronato, Sinop-MT, Brazil.

Drug Development and Industrial Pharmacy
|November 15, 2011
PubMed
Summary

This study improved β-lapachone (βLAP) dissolution for Chagas disease treatment by adsorbing it onto microcrystalline cellulose. Resulting βLAP powder and tablets show enhanced dissolution rates for oral administration.

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Natural Product Chemistry

Background:

  • β-lapachone (βLAP), a natural compound, shows potent antichagasic activity by generating free radicals and inhibiting nucleic acid and protein synthesis.
  • Key challenges for βLAP development include its low water solubility and the need for large therapeutic doses.
  • Overcoming these limitations is crucial for effective Chagas disease treatment.

Purpose of the Study:

  • To enhance the limited dissolution rate of β-lapachone (βLAP).
  • To achieve this by promoting spontaneous crystalline growth of βLAP on an inert excipient surface.
  • To develop improved oral dosage forms of βLAP.

Main Methods:

  • Physicochemical characterization of βLAP-adsorbed particles.
  • Assessment of drug dissolution rates for adsorbed particles, raw drug, and physical mixtures.
  • Evaluation of βLAP-adsorbed particle utility in directly compressed tablets.

Main Results:

  • Spontaneous crystalline growth of βLAP on microcrystalline cellulose (MCC) resulted in particles with fast dissolution rates (90% dissolved within 50 minutes).
  • No physical or chemical instability of βLAP was observed post-adsorption.
  • Direct compression into tablets maintained good dissolution behavior with appropriate pressure.

Conclusions:

  • Surface adsorption is a simple method to produce βLAP powder with enhanced dissolution.
  • This technique facilitates the development of βLAP tablets for improved oral administration.
  • The findings offer a promising strategy for developing effective oral Chagas disease therapies.