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Polymerized phospholipid vesicles containing amphotericin B: evaluation of toxic and antifungal activities in vitro
Abstract:
We have prepared lipid vesicles (liposomes) composed of polymerized bis[12-(methacryloyloxy)dodecanoyl]-L-alpha-phosphatidylcholine (DPL) which contain the antifungal polyene antibiotic amphotericin B (AMB). It was necessary to devise a novel method for incorporating AMB into the liposomes subsequent to polymerization. The polymer liposome AMB was as effective as AMB in "conventional" liposomes in terms of inhibiting fungal growth in vitro. However, in contrast to "conventional" liposomes, the polymerized DPL vesicles did not protect mammalian cells against AMB induced toxicity.
Insights
Polymerized liposomes containing amphotericin B (AMB) effectively inhibit fungal growth. However, these novel polymer liposomes fail to protect mammalian cells from AMB toxicity, unlike conventional liposomes.
Area of Science:
- Biochemistry
- Polymer Chemistry
- Pharmacology
Background:
- Amphotericin B (AMB) is a potent antifungal polyene antibiotic.
- Conventional liposomes are used to encapsulate AMB, improving its therapeutic index.
- Polymerized lipid vesicles offer potential advantages in drug delivery stability.
Purpose of the Study:
- To develop and characterize polymerized lipid vesicles (liposomes) containing AMB.
- To investigate a novel method for incorporating AMB into liposomes post-polymerization.
- To evaluate the efficacy and toxicity of polymer liposome AMB compared to conventional liposomes.
Main Methods:
- Preparation of liposomes from polymerized bis[12-(methacryloyloxy)dodecanoyl]-L-alpha-phosphatidylcholine (DPL).
- Development of a novel post-polymerization method for AMB incorporation.
- In vitro assessment of antifungal activity against fungal growth.
- Evaluation of mammalian cell protection against AMB-induced toxicity.
Main Results:
- Polymer liposome AMB demonstrated comparable in vitro antifungal efficacy to conventional liposome AMB.
- Polymerized DPL vesicles containing AMB did not provide protection to mammalian cells.
- Conventional liposomes offered protection to mammalian cells against AMB toxicity.
Conclusions:
- Novel polymerized liposomes can encapsulate AMB with retained antifungal activity.
- The polymerized DPL vesicles lack the cytoprotective properties observed with conventional liposomes.
- Further research is needed to optimize polymer liposome formulations for improved safety profiles.