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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...
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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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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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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.
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Formation of Dispersible Taohong Siwu Tablets
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Design and optimization of ganciclovir solid dispersion for improving its bioavailability.

Dalia A Gaber1,2, Manar A Alnwiser3, Nadia L Alotaibi3

  • 1Department of Pharmaceutics, College of Pharmacy, AL-Qassim University, Qassim, KSA.

Drug Delivery
|June 8, 2022
PubMed
Summary

New nano Ganciclovir (GC) particles enhance oral drug delivery. This solid dispersion technique significantly boosts GC bioavailability by over twofold compared to conventional tablets.

Keywords:
Gancyclovircyclodextrinfactorial designnanoparticlesshellacsolid dispersion

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Area of Science:

  • Pharmaceutical Sciences
  • Nanotechnology in Drug Delivery
  • Biopharmaceutics

Background:

  • Ganciclovir (GC) is a Class III antiviral drug with poor oral absorption, limiting its therapeutic efficacy.
  • Nanoparticle encapsulation can improve the permeability and bioavailability of poorly soluble drugs.
  • Developing advanced oral delivery systems is crucial for enhancing antiviral drug performance.

Purpose of the Study:

  • To develop and optimize nanosized solid dispersion particles of Ganciclovir (GC) using cyclodextrin and shellac.
  • To enhance the permeability, release pattern, and oral bioavailability of Ganciclovir.
  • To evaluate the physicochemical properties, in vitro release, stability, and in vivo pharmacokinetics of the optimized formulation.

Main Methods:

  • Ganciclovir was incorporated into nanosized particles using the solvent evaporation technique with cyclodextrin and shellac.
  • A 2^3 full factorial design was employed to optimize formulation variables.
  • Characterization included particle size, zeta potential, drug content, micromeritics, DSC, FTIR, in vitro release, stability studies, and in vivo pharmacokinetic evaluation in rabbits.

Main Results:

  • The optimized formulation (F6) exhibited a mean particle size of 288.5 nm, zeta potential of 23.87, and drug content of 95.77%.
  • In vitro release showed an initial burst followed by sustained release over 12 hours.
  • In vivo studies in rabbits demonstrated a 2.2-fold increase in Ganciclovir bioavailability compared to conventional tablets, with good stability over 6 months.

Conclusions:

  • The developed nano Ganciclovir solid dispersion particles successfully enhanced oral permeability and bioavailability.
  • The solvent evaporation technique combined with cyclodextrin and shellac is effective for improving Ganciclovir's pharmacokinetic profile.
  • This approach offers a promising strategy for improving the oral delivery of poorly absorbed antiviral drugs like Ganciclovir.