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07:32
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Human pancreatic polypeptide in a phospholipid-based micellar formulation.
Amrita Banerjee1, Hayat Onyuksel
1Department of Biopharmaceutical Sciences, University of Illinois at Chicago, Chicago, Illinois 60612, USA.
Pharmaceutical Research
|March 9, 2012
Summary
Pancreatic polypeptide (PP) formulated in sterically stabilized micelles (SSM) overcomes its short half-life and aggregation issues. This stabilized PP formulation shows improved stability and retains bioactivity, offering a promising therapeutic for diabetes.
Area of Science:
- Biochemistry
- Nanomedicine
- Pharmacology
Background:
- Pancreatic polypeptide (PP) possesses crucial glucoregulatory functions, making it a potential therapeutic agent for diabetes and obesity.
- Therapeutic application of PP is hindered by its short plasma half-life and tendency to aggregate in aqueous solutions.
- Sterically stabilized micelles (SSM) offer a potential solution for stabilizing peptides and improving their delivery.
Purpose of the Study:
- To develop and characterize a formulation of pancreatic polypeptide (PP) encapsulated in sterically stabilized micelles (SSM).
- To enhance the stability and therapeutic applicability of PP by protecting it from degradation and aggregation.
- To evaluate the feasibility of long-term storage and in vitro bioactivity of the PP-SSM formulation.
Main Methods:
- PP was incubated with SSM dispersion in phosphate buffers with or without sodium chloride.
- Dynamic light scattering, fluorescence spectroscopy, and circular dichroism were used to characterize peptide-micelle association and formulation stability.
- High-performance liquid chromatography (HPLC) assessed proteolytic degradation, and in vitro cAMP inhibition studies evaluated bioactivity.
Main Results:
- PP demonstrated self-association with SSM, with interaction influenced by sodium chloride presence.
- The PP-SSM formulation was successfully lyophilized, indicating suitability for long-term storage.
- The formulation significantly improved PP's stability against proteolytic degradation while preserving its in vitro bioactivity.
Conclusions:
- Self-association of PP with phospholipid micelles effectively addresses previous delivery challenges.
- The developed nanomedicine formulation shows promise for the treatment of diabetes.
- Further development of this PP-SSM nanomedicine is warranted for clinical applications.
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