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[A basic study on usefulness of bleomycin incorporated in poly DL-lactic acid]
T Kumanohoso1, S Natsugoe, M Shimada
1First Dept. of Surgery, Kagoshima University School of Medicine.
Gan to Kagaku Ryoho. Cancer & Chemotherapy
|August 1, 1993
Summary
Poly DL-lactic acid (PLA) effectively delivers bleomycin (BLM) as a sustained-release anti-cancer drug. This new BLM-PLA formulation shows promise for local chemotherapy with minimal systemic drug exposure.
Area of Science:
- Biomaterials Science
- Pharmacology
- Drug Delivery Systems
Background:
- Poly DL-lactic acid (PLA) is a biodegradable polymer with potential applications in drug delivery.
- Developing novel drug formulations is crucial for effective cancer treatment.
- Bleomycin (BLM) is an anti-cancer drug requiring controlled release mechanisms.
Purpose of the Study:
- To develop and evaluate a new dosage form of bleomycin (BLM) using Poly DL-lactic acid (PLA) blends.
- To assess the in vitro dissolution profile of BLM from the BLM-PLA formulation.
- To investigate the in vivo distribution and BLM activity following subcutaneous implantation of BLM-PLA in rats.
Main Methods:
- Preparation of BLM-PLA composite cylinders.
- In vitro dissolution testing of BLM-PLA in saline.
- Subcutaneous implantation of BLM-PLA in rats and subsequent measurement of BLM activity in various tissues (connective tissue, lymph node, lung, liver, kidney) over 35 days.
Main Results:
- In vitro, BLM dissolution from BLM-PLA reached 49.2% at 7 days, 85.2% at 14 days, and 99.7% at 21 days.
- In vivo, high BLM concentrations were sustained in connective tissues for 14 days and in lymph nodes for 21-28 days.
- Low BLM levels were observed in the lung, liver, and kidney, indicating localized drug action.
Conclusions:
- PLA serves as an effective carrier for a drug delivery system.
- The BLM-PLA formulation demonstrates potential as an effective anti-cancer modality, particularly for local chemotherapy.
- The localized drug delivery minimizes systemic exposure, suggesting improved therapeutic index.