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Injectable PLA-based in situ forming implants for controlled release of Ivermectin a BCS Class II drug: solvent
J A Camargo1, A Sapin, C Nouvel
1Faculty of Pharmacy, Laboratory of Pharmaceutical Technology, Nancy University, EA 3452 Nancy Cedex, France.
Drug Development and Industrial Pharmacy
|March 9, 2012
Summary
Biocompatible solvents significantly impact drug release from in situ forming implants (ISI). Solvent water miscibility and viscosity control ivermectin release rates and implant porosity, influencing antiparasitic efficacy.
Area of Science:
- Biomaterials Science
- Pharmaceutical Technology
- Drug Delivery Systems
Background:
- In situ forming implants (ISI) offer sustained drug release via parenteral administration using biodegradable polymers like poly(D,L-lactide) (PLA).
- Optimizing ISI performance requires understanding the influence of biocompatible solvents on drug release kinetics and drug/polymer stability.
Purpose of the Study:
- To investigate the effect of various biocompatible solvents (NMP, 2P, TA, BB) on the release of ivermectin (IVM) from PLA-based ISI.
- To correlate solvent physico-chemical properties with drug release rates, implant microstructure, and the stability of both PLA and IVM.
Main Methods:
- Preparation of PLA-based ISI loaded with ivermectin (IVM).
- Evaluation of solvent properties (Hansen's solubility parameters, water miscibility, viscosity) and their interaction with PLA.
- Quantification of IVM release kinetics using high-performance liquid chromatography (HPLC).
- Analysis of implant morphology (surface porosity) via scanning electron microscopy (SEM).
- Assessment of PLA and IVM stability in different solvents.
Main Results:
- IVM release rate was primarily governed by solvent water miscibility and polymer solution viscosity.
- Release rates followed the order: NMP > 2P > TA > BB, correlating with increasing water miscibility and decreasing viscosity.
- Increased implant surface porosity, observed with higher release rates, was linked to solvent properties.
- PLA and IVM stability generally increased with decreased polymer-solvent affinity and lower solvent water content.
- IVM degradation was accelerated by the acidic environment from PLA degradation, but IVM did not affect PLA stability.
Conclusions:
- Solvent selection is critical for controlling ivermectin release kinetics from PLA-based ISI.
- Water miscibility and viscosity of biocompatible solvents are key parameters for tuning drug release and implant characteristics.
- Understanding these solvent-drug-polymer interactions is essential for designing effective sustained-release formulations.
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