Abstract
Background: Many different methods have been developed to incorporate hydrophobic compounds into polymeric micelles, including simple equilibrium (SE) and solvent casting (SC). Thus far, no studies have compared the SE and SC methods for drug loading and stability.
Methods: Resveratrol (RES), a model hydrophobic compound, loaded in various Pluronics® (F88, F98, F108, and F127) is used to determine the differences between SE and SC methods.
Results: Micelles prepared by SE method demonstrated RES loading in proportion to their respective CMC values with F127 having the lowest CMC and highest loading at Day 14 of 5.39±0.19 mg/mL, followed by F98 at 3.65±0.13 mg/mL, F108 at 3.29±0.06, and F88 at 2.35±0.05 mg/mL. Initial RES loading in SC method approaches 10 mg/mL in all the polymers, however, the micelles are unable to retain RES at this concentration for more than a few hours to a day. At the lower loading of 5 mg/mL a higher stability is seen in the Pluronic® micelles. In all micelles prepared by SC method, whether high or low loading, over a 14 day period the RES concentration in the micelles approached the equilibrium RES solubility.
Conclusion: Our results demonstrate that micelles prepared by SC result in meta-stable micelles when the amount of the compound loaded exceeds the equilibrium loading and the rate at which the compound in the micelles approaches equilibrium solubility is determined by the hydrophobicity of the compound and the hydrophile- lipophile balance (HLB) of the polymer.
Keywords: Drug loading and retention, micelle stability, pluronics®, polymeric micelles, resveratrol, simple equilibrium method, solvent casting method.
Graphical Abstract
Pharmaceutical Nanotechnology
Title:Evaluation of the Stability of Resveratrol Pluronic® Micelles Prepared by Solvent Casting and Simple Equilibrium Methods
Volume: 4 Issue: 2
Author(s): Deepa A. Rao, Brianna Cote, Michelle Stammet, Adel M. Al Fatease and Adam W.G. Alani
Affiliation:
Keywords: Drug loading and retention, micelle stability, pluronics®, polymeric micelles, resveratrol, simple equilibrium method, solvent casting method.
Abstract: Background: Many different methods have been developed to incorporate hydrophobic compounds into polymeric micelles, including simple equilibrium (SE) and solvent casting (SC). Thus far, no studies have compared the SE and SC methods for drug loading and stability.
Methods: Resveratrol (RES), a model hydrophobic compound, loaded in various Pluronics® (F88, F98, F108, and F127) is used to determine the differences between SE and SC methods.
Results: Micelles prepared by SE method demonstrated RES loading in proportion to their respective CMC values with F127 having the lowest CMC and highest loading at Day 14 of 5.39±0.19 mg/mL, followed by F98 at 3.65±0.13 mg/mL, F108 at 3.29±0.06, and F88 at 2.35±0.05 mg/mL. Initial RES loading in SC method approaches 10 mg/mL in all the polymers, however, the micelles are unable to retain RES at this concentration for more than a few hours to a day. At the lower loading of 5 mg/mL a higher stability is seen in the Pluronic® micelles. In all micelles prepared by SC method, whether high or low loading, over a 14 day period the RES concentration in the micelles approached the equilibrium RES solubility.
Conclusion: Our results demonstrate that micelles prepared by SC result in meta-stable micelles when the amount of the compound loaded exceeds the equilibrium loading and the rate at which the compound in the micelles approaches equilibrium solubility is determined by the hydrophobicity of the compound and the hydrophile- lipophile balance (HLB) of the polymer.
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A. Rao Deepa, Cote Brianna, Stammet Michelle, M. Al Fatease Adel and W.G. Alani Adam, Evaluation of the Stability of Resveratrol Pluronic® Micelles Prepared by Solvent Casting and Simple Equilibrium Methods, Pharmaceutical Nanotechnology 2016; 4 (2) . https://dx.doi.org/10.2174/2211738504666160428155355
DOI https://dx.doi.org/10.2174/2211738504666160428155355 |
Print ISSN 2211-7385 |
Publisher Name Bentham Science Publisher |
Online ISSN 2211-7393 |
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