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Solidified mPEG-PDLLA micelles as a novel oral delivery system of indomethacin

Ouahab Ammar1, Yan Shen, Qi-Neng Ping

  • 1Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China.

Yao Xue Xue Bao = Acta Pharmaceutica Sinica
|October 20, 2011
PubMed

Insights

Solidified-polymeric micelles effectively encapsulate indomethacin (IND), enhancing its solubility. These IND-loaded micelles show rapid dissolution, making them suitable for tablet and capsule formulations.

Area of Science:

  • Pharmaceutical Technology
  • Materials Science
  • Drug Delivery Systems

Background:

  • Indomethacin (IND) is a nonsteroidal anti-inflammatory drug with limited aqueous solubility.
  • Developing effective drug delivery systems is crucial for improving IND bioavailability and therapeutic efficacy.
  • Polymeric micelles offer a promising platform for encapsulating hydrophobic drugs like IND.

Purpose of the Study:

  • To prepare and characterize indomethacin-loaded solidified-polymeric micelles (IND-SPM).
  • To evaluate the in vitro dissolution properties and solubility enhancement of IND.
  • To assess the suitability of IND-SPM for pharmaceutical formulations such as tablets and capsules.

Main Methods:

  • IND-SPM were prepared using a solution-absorption method followed by rotary evaporation.
  • Methoxy-poly(ethylene glycol)-poly(D, L-lactide) copolymer (mPEG-PDLLA) was utilized as the drug carrier.
  • Polyplasdone XL-10 served as an adsorbent during the preparation process.

Main Results:

  • Over 90% of IND dissolved within 30 minutes from the IND-SPM powder in PBS.
  • Differential Scanning Calorimetry (DSC), 1H Nuclear Magnetic Resonance (NMR), and Scanning Electron Microscopy (SEM) confirmed IND encapsulation within mPEG-PDLLA.
  • A 4.6-fold increase in IND solubility was observed at the highest copolymer concentration.

Conclusions:

  • The prepared IND-SPM demonstrated excellent in vitro dissolution characteristics.
  • The mPEG-PDLLA copolymer effectively encapsulated IND, significantly enhancing its solubility.
  • IND-SPM are suitable for the development of solid dosage forms like tablets and capsules.

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