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The encapsulation of bleomycin within chitosan based polymeric vesicles does not alter its biodistribution
J Sludden1, I F Uchegbu, A G Schätzlein
1CRC Department of Medical Oncology, University of Glasgow, UK.
The Journal of Pharmacy and Pharmacology
|May 17, 2000
Summary
Palmitoyl glycol chitosan (GCP41) vesicles were evaluated as a drug delivery system for bleomycin. These polymeric vesicles showed plasma instability in vivo, limiting their therapeutic potential.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Drug Delivery
Background:
- Polymeric vesicles offer potential for drug delivery applications.
- Amphiphilic chitosan derivatives are being explored for vesicle formulation.
Purpose of the Study:
- To evaluate the potential of palmitoyl glycol chitosan (GCP41) vesicles as a drug delivery system.
- To assess the stability and drug release characteristics of GCP41 vesicles using bleomycin as a model drug.
Main Methods:
- Synthesis of palmitoyl glycol chitosan (GCP41).
- Preparation of bleomycin-loaded GCP41 vesicles via remote loading and extrusion.
- In vitro stability testing in plasma and drug release studies.
- In vivo biodistribution studies in male Balb/c mice.
Main Results:
- GCP41 vesicles (669 nm) showed a 49% size reduction upon in vitro plasma incubation.
- Both GCP41 and control niosomes retained approximately 62-63% of bleomycin after 24h.
- Extruded GCP41 vesicles (290 nm) did not significantly alter bleomycin pharmacokinetics in mice, with slight increases in plasma and kidney levels.
Conclusions:
- Extruded GCP41 vesicles degrade in plasma in vivo.
- The observed plasma instability suggests limited therapeutic advantage over free bleomycin for this formulation.