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Related Concept Videos

Drug Delivery: Overview01:16

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The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
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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...
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Acacetin-loaded microemulsion for transdermal delivery: preparation, optimization and evaluation.

Yajing Wang1, Qian Chen1, Xianfeng Huang1

  • 1Department of Pharmacy, Changzhou University, Changzhou, PR China.

Pharmaceutical Biology
|May 10, 2023
PubMed
Summary

This study developed acacetin-loaded microemulsions for transdermal delivery, significantly improving drug solubility and absorption. This offers a promising non-invasive treatment option for atrial fibrillation.

Keywords:
Emulsionspermeation enhancerspharmacokineticssimplex lattice experiment designsolubility

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Nanotechnology

Background:

  • Acacetin shows potential for treating atrial fibrillation.
  • Clinical use is hindered by poor solubility and low oral bioavailability.

Purpose of the Study:

  • To prepare and evaluate acacetin-loaded microemulsions (ME) for enhanced transdermal delivery.
  • To improve acacetin's pharmacokinetic profile and enable non-invasive administration.

Main Methods:

  • Microemulsion formulation optimized using water titration and simplex lattice design.
  • Ex vivo skin permeation studies using Franz diffusion cells.
  • In vivo pharmacokinetic studies in rats following transdermal administration.

Main Results:

  • Optimized ME (FA) exhibited small particle size (36.0 nm) and high drug solubility (803.7 mg/g).
  • Formulations with penetration enhancers (FB) showed significantly higher cumulative drug permeation and AUC0-∞ compared to controls.
  • Transdermal administration achieved efficient pharmacokinetics within 6 hours.

Conclusions:

  • Microemulsion formulation combined with penetration enhancers effectively improves acacetin solubility and percutaneous absorption.
  • This approach provides a viable non-invasive delivery strategy for acacetin.
  • Offers a new therapeutic option for atrial fibrillation treatment.