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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Bioavailability effect of methylprednisolone by polymeric micelles
Ching-Lin Chen1, Shwu-Fen Chang, Daniel Lee
1Neurosurgical Department, Shin Kong Wu Ho-Su Memorial Hospital, Shih Lin District, Taipei, Taiwan.
Polymeric micelles (PM) enhance methylprednisolone (MP) delivery for spinal cord injury (SCI) treatment. This formulation improves MP bioavailability in blood and spinal cord, increasing the anti-apoptotic marker Bcl-x(L) expression.
Area of Science:
- Pharmacology
- Biomaterials Science
- Neuroscience
Background:
- Methylprednisolone (MP) is a treatment for spinal cord injury (SCI).
- Improving MP bioavailability to the blood and spinal cord (SC) is crucial for effective treatment.
- Polymeric micelles (PM) offer a potential drug delivery system to enhance therapeutic efficacy.
Purpose of the Study:
- To investigate the effect of PEO-PPO-PEO polymeric micelles (PM) formulation on the bioavailability of methylprednisolone (MP).
- To assess the impact of PM on MP delivery to the blood and spinal cord (SC) in rabbits.
- To evaluate the influence of PM-formulated MP on the expression of the anti-apoptotic marker Bcl-x(L).
Main Methods:
- Characterization of MP formulated with PM (MP/PM) using CMC, DLS, AFM, and in vitro release studies.
- Analysis of MP disposition in plasma and SC of rabbits via HPLC after intravenous administration.
- Monitoring of Bcl-x(L) mRNA and protein levels using RT-qPCR and Western blotting, respectively.
Main Results:
- PEO-PPO-PEO copolymers formed micelles, with MP/PM exhibiting an average size of 60 nm.
- MP/PM formulation demonstrated enhanced solubility and release rate compared to MP alone.
- Intravenous administration of MP/PM significantly increased MP levels and half-life in plasma and SC.
- MP/PM administration led to a 4-fold increase in Bcl-x(L) mRNA and elevated protein levels in the SC.
Conclusions:
- PM formulation effectively improves the pharmacokinetic profile of MP in both plasma and SC.
- The PM vehicle enhances MP delivery, leading to increased expression of the anti-apoptotic marker Bcl-x(L).
- This study highlights the potential of PM as a drug delivery system for SCI treatment.
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