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Drug-polyionic block copolymer interactions for micelle formation: physicochemical characterisation.

T Govender¹, S Stolnik, C Xiong

¹School of Pharmacy and Pharmacology, University of Durban-Westville, Private Bag, X54001, Durban, South Africa.

Journal of Controlled Release : Official Journal of the Controlled Release Society

|August 8, 2001

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This study demonstrates that non-covalent interactions between Poly(aspartic acid)-poly(ethylene glycol) (Pasp-PEG) and diminazene aceturate can form stable polyionic micelles for drug delivery. These micelles show potential for enhanced therapeutic applications.

Area of Science:

Polymer Chemistry
Materials Science
Nanotechnology

Background:

Covalent drug attachment to polymeric micelles is common, but non-covalent methods are less explored.
Polymeric micelles offer advantages in drug delivery systems.
Poly(aspartic acid)-poly(ethylene glycol) (Pasp-PEG) is an AB copolymer with potential for micelle formation.

Purpose of the Study:

To investigate non-covalent interactions between Pasp-PEG and diminazene aceturate for polyionic micelle formation.
To characterize the properties of these self-assembled micelles for drug delivery applications.

Main Methods:

Preparation of micelles by mixing Pasp-PEG and diminazene aceturate in buffer.
Characterization of micelle size, zeta potential, and stability using dynamic light scattering and zeta potential measurements.

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Assessment of pH and salt effects on micelle properties.

Isothermal titration microcalorimetry to evaluate binding interactions.

Morphological evaluation using microscopy.

Main Results:

Water-soluble micelles with unimodal size distribution (22-60 nm) were formed.
Micelles exhibited small zeta potential, indicating PEG corona stabilization.
Particle size and scattering intensity were stable within a pH range of 3.4-7.2.
Increased NaCl concentration led to micelle aggregation due to PEG corona dehydration.
Isothermal titration microcalorimetry confirmed dominant hydrogen bonding, ensuring micellar stability against salt-induced dissociation.
Morphological evaluation showed discrete and uniform micelles.

Conclusions:

Non-covalent interactions between Pasp-PEG and diminazene aceturate successfully form stable polyionic micelles.
These micelles demonstrate potential as a drug delivery system.
The study highlights the efficacy of hydrogen bonding in stabilizing polyionic micelles against dissociation.