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Modified-Release Drug Delivery Systems: Bioavailability01:30

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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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Rate-programmed drug delivery systems (DDS) are designed to release drugs at specific, controlled rates to maintain consistent therapeutic levels. These systems are categorized based on their release mechanisms, including dissolution-controlled DDS, diffusion-controlled DDS, and combined dissolution-diffusion-controlled DDS.In dissolution-controlled DDS, the release rate depends on the slow dissolution of the drug itself or the surrounding matrix. Drugs with inherently slow dissolution rates,...
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Alternative drug dissolution methods include the rotating bottle, intrinsic dissolution test, peristalsis, and the Franz diffusion cell method. The rotating bottle method involves meticulously rotating tightly capped controlled-release beads in a temperature-controlled bath. Periodic decanting of samples allows for residue assay, followed by refilling with fresh medium and testing at various pH levels to emulate the gastrointestinal tract conditions.In contrast, the intrinsic dissolution test...
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Modified-release drug delivery systems are designed to optimize the therapeutic effect of drugs by minimizing side effects, reducing the dosage required, and controlling drug release to align with pharmacokinetic and pharmacodynamic needs. The system depends on two key factors: the drug's release from the formulation and its movement through the body to the target site. Unlike conventional dosage forms, where absorption is the limiting step, the rate of drug release is the key determinant in...
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In vitro dissolution and drug release tests assess how quickly and how much of a drug is released from its dosage form into an aqueous medium under standardized laboratory conditions. These tests are essential tools in pharmaceutical development and quality assurance, offering insight into the drug's performance before clinical use.During formulation development, dissolution testing identifies incomplete or inconsistent drug release issues. It also supports decisions on selecting the optimal...
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Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells
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In vitro controlled release of Rifampicin through liquid-crystalline folate nanoparticles.

Rohan Parmar1, Rahul Misra1, Sanat Mohanty1

  • 1Department of Chemical Engineering, Indian Institute of Technology-Delhi, Hauz Khas, New Delhi 110016, India.

Colloids and Surfaces. B, Biointerfaces
|April 13, 2015
PubMed
Summary

Researchers developed novel liquid-crystalline folate nanoparticles for sustained Rifampicin delivery, improving tuberculosis treatment. These nanoparticles offer controlled release and enhanced drug bioavailability, addressing a key concern in combination therapy.

Keywords:
Alveolar macrophageControl releaseLiquid-crystalline folateRifampicinTuberculosis

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Area of Science:

  • Nanotechnology
  • Pharmacology
  • Materials Science

Background:

  • Rifampicin is a primary tuberculosis drug, but its efficacy is limited by poor bioavailability in combination therapies.
  • Nano-based drug delivery systems show promise for enhancing the pharmacokinetic behavior and antibacterial efficacy of anti-tubercular agents.
  • Developing advanced formulations is crucial to overcome challenges in tuberculosis treatment.

Purpose of the Study:

  • To design and characterize liquid-crystalline folate nanoparticles for sustained delivery of Rifampicin.
  • To investigate the in vitro release kinetics of Rifampicin from these novel nanoparticles.
  • To evaluate the potential of these nanoparticles for improved tuberculosis therapy.

Main Methods:

  • Synthesis of liquid-crystalline folate nanoparticles encapsulating Rifampicin.
  • In vitro release studies to determine drug release profiles over time.
  • Investigation of parameters influencing Rifampicin release, including nanoparticle size and cross-linking conditions.
  • Assessment of nanoparticle uptake and cytotoxicity in alveolar macrophages using fluorescence microscopy and MTT assay.

Main Results:

  • Liquid-crystalline folate nanoparticles demonstrated high encapsulation efficiency and controlled release of Rifampicin.
  • Sustained drug release was observed for over 25 days.
  • Nanoparticle size, cross-linking cation type and concentration, and drug-loading significantly impacted Rifampicin release profiles.
  • Demonstrated intracellular uptake and low cytotoxicity of the nanoparticles in alveolar macrophages.

Conclusions:

  • Liquid-crystalline folate nanoparticles represent a promising platform for sustained Rifampicin delivery.
  • This formulation can potentially improve the pharmacokinetic profile and therapeutic efficacy of Rifampicin in tuberculosis treatment.
  • Further research into these nanoparticles could lead to advanced anti-tubercular drug delivery strategies.