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Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration.

Li J, Li Z, Zhou T, Zhang J, Xia H, Li H, He J, He S, Wang L - Int J Nanomedicine (2015)

Bottom Line: The polymer was successfully synthesized and confirmed using nuclear magnetic resonance and Fourier transform infrared.The drug-loading efficiency and drug-loading content were 75.37% and 3.47%, respectively, which indicates that the polymeric micelles possess a high drug-loading capacity.Positively charged micelles generated from a triblock copolymer are a promising vehicle for the topical delivery of hydrophobic agents in ocular applications.

View Article: PubMed Central - PubMed

Affiliation: Henan Eye Institute, Henan Eye Hospital, Henan Provincial People's Hospital and Zhengzhou University People's Hospital, Zhengzhou, People's Republic of China.

ABSTRACT

Purpose: The cornea is a main barrier to drug penetration after topical application. The aim of this study was to evaluate the abilities of micelles generated from a positively charged triblock copolymer to penetrate the cornea after topical application.

Methods: The triblock copolymer poly(ethylene glycol)-poly(ε-caprolactone)-g-polyethyleneimine was synthesized, and the physicochemical properties of the self-assembled polymeric micelles were investigated, including hydrodynamic size, zeta potential, morphology, drug-loading content, drug-loading efficiency, and in vitro drug release. Using fluorescein diacetate as a model drug, the penetration capabilities of the polymeric micelles were monitored in vivo using a two-photon scanning fluorescence microscopy on murine corneas after topical application.

Results: The polymer was successfully synthesized and confirmed using nuclear magnetic resonance and Fourier transform infrared. The polymeric micelles had an average particle size of 28 nm, a zeta potential of approximately +12 mV, and a spherical morphology. The drug-loading efficiency and drug-loading content were 75.37% and 3.47%, respectively, which indicates that the polymeric micelles possess a high drug-loading capacity. The polymeric micelles also exhibited controlled-release behavior in vitro. Compared to the control, the positively charged polymeric micelles significantly penetrated through the cornea.

Conclusion: Positively charged micelles generated from a triblock copolymer are a promising vehicle for the topical delivery of hydrophobic agents in ocular applications.

No MeSH data available.


Related in: MedlinePlus

Schematic illustration of the formation of drug-loaded polymeric micelles.Abbreviations: PEG, poly(ethylene glycol); PCL, poly(ε-caprolactone); PEI, polyethyleneimine.
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f4-ijn-10-6027: Schematic illustration of the formation of drug-loaded polymeric micelles.Abbreviations: PEG, poly(ethylene glycol); PCL, poly(ε-caprolactone); PEI, polyethyleneimine.

Mentions: As an amphiphilic block copolymer, mPEG-PCL-g-PEI can self-assemble into polymeric micelles in an aqueous phase with a positive charge.28 These cationic nanomicelles can be loaded with hydrophobic drugs; a schematic illustration is shown in Figure 4. The sizes and zeta potentials of the polymeric micelles were determined via dynamic light scattering, and the results are shown in Table 1. The micelles had a relatively small average hydrodynamic diameter of 27.74 nm, a PDI of 0.212, and a moderate positive charge of 12.12 mV. The morphology of the polymeric micelles was determined by SEM and appeared to be uniform and spherical in shape (Figure 5A).


Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration.

Li J, Li Z, Zhou T, Zhang J, Xia H, Li H, He J, He S, Wang L - Int J Nanomedicine (2015)

Schematic illustration of the formation of drug-loaded polymeric micelles.Abbreviations: PEG, poly(ethylene glycol); PCL, poly(ε-caprolactone); PEI, polyethyleneimine.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4592048&req=5

f4-ijn-10-6027: Schematic illustration of the formation of drug-loaded polymeric micelles.Abbreviations: PEG, poly(ethylene glycol); PCL, poly(ε-caprolactone); PEI, polyethyleneimine.
Mentions: As an amphiphilic block copolymer, mPEG-PCL-g-PEI can self-assemble into polymeric micelles in an aqueous phase with a positive charge.28 These cationic nanomicelles can be loaded with hydrophobic drugs; a schematic illustration is shown in Figure 4. The sizes and zeta potentials of the polymeric micelles were determined via dynamic light scattering, and the results are shown in Table 1. The micelles had a relatively small average hydrodynamic diameter of 27.74 nm, a PDI of 0.212, and a moderate positive charge of 12.12 mV. The morphology of the polymeric micelles was determined by SEM and appeared to be uniform and spherical in shape (Figure 5A).

Bottom Line: The polymer was successfully synthesized and confirmed using nuclear magnetic resonance and Fourier transform infrared.The drug-loading efficiency and drug-loading content were 75.37% and 3.47%, respectively, which indicates that the polymeric micelles possess a high drug-loading capacity.Positively charged micelles generated from a triblock copolymer are a promising vehicle for the topical delivery of hydrophobic agents in ocular applications.

View Article: PubMed Central - PubMed

Affiliation: Henan Eye Institute, Henan Eye Hospital, Henan Provincial People's Hospital and Zhengzhou University People's Hospital, Zhengzhou, People's Republic of China.

ABSTRACT

Purpose: The cornea is a main barrier to drug penetration after topical application. The aim of this study was to evaluate the abilities of micelles generated from a positively charged triblock copolymer to penetrate the cornea after topical application.

Methods: The triblock copolymer poly(ethylene glycol)-poly(ε-caprolactone)-g-polyethyleneimine was synthesized, and the physicochemical properties of the self-assembled polymeric micelles were investigated, including hydrodynamic size, zeta potential, morphology, drug-loading content, drug-loading efficiency, and in vitro drug release. Using fluorescein diacetate as a model drug, the penetration capabilities of the polymeric micelles were monitored in vivo using a two-photon scanning fluorescence microscopy on murine corneas after topical application.

Results: The polymer was successfully synthesized and confirmed using nuclear magnetic resonance and Fourier transform infrared. The polymeric micelles had an average particle size of 28 nm, a zeta potential of approximately +12 mV, and a spherical morphology. The drug-loading efficiency and drug-loading content were 75.37% and 3.47%, respectively, which indicates that the polymeric micelles possess a high drug-loading capacity. The polymeric micelles also exhibited controlled-release behavior in vitro. Compared to the control, the positively charged polymeric micelles significantly penetrated through the cornea.

Conclusion: Positively charged micelles generated from a triblock copolymer are a promising vehicle for the topical delivery of hydrophobic agents in ocular applications.

No MeSH data available.


Related in: MedlinePlus