Limits...
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

Synthetic route of the copolymer.Abbreviations: ε-CL, ε-caprolactone; PEI, polyethyleneimine; DCC, dicyclohexylcarbodiimide; NHS, N-hydroxy-succinimide; PEG-PCL-g-PEI, poly(ethylene glycol)-poly (ε-caprolactone)-g-polyethyleneimine.
© Copyright Policy
Related In: Results  -  Collection

License
getmorefigures.php?uid=PMC4592048&req=5

f1-ijn-10-6027: Synthetic route of the copolymer.Abbreviations: ε-CL, ε-caprolactone; PEI, polyethyleneimine; DCC, dicyclohexylcarbodiimide; NHS, N-hydroxy-succinimide; PEG-PCL-g-PEI, poly(ethylene glycol)-poly (ε-caprolactone)-g-polyethyleneimine.

Mentions: The triblock copolymer PCI was synthesized via a combination of ring-opening polymerization of ε-CL and an amidation reaction between the amine group of PEI and the carboxyl group of PCL, as outlined in Figure 1. The chemical structures of the copolymers were confirmed by 1H NMR and FTIR spectroscopy. In Figure 2, the 1H NMR spectra of the triblock copolymer PCI and the propolymer clearly show characteristic resonance peaks of PEG, PCL, and PEI. The sharp peak appearing at 3.64 ppm was attributed to the methylene protons in the PEG blocks. The typical signals of the methylene protons in the PCL blocks appeared at 1.32 ppm, 1.56 ppm, 2.31 ppm, and 4.06 ppm. The strong and broad absorption peaks that were observed at 2.5–2.9 ppm were assigned to the methane protons of PEI.27 The 1H NMR results showed that the PCI copolymer was successfully synthesized.


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)

Synthetic route of the copolymer.Abbreviations: ε-CL, ε-caprolactone; PEI, polyethyleneimine; DCC, dicyclohexylcarbodiimide; NHS, N-hydroxy-succinimide; PEG-PCL-g-PEI, poly(ethylene glycol)-poly (ε-caprolactone)-g-polyethyleneimine.
© Copyright Policy
Related In: Results  -  Collection

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

f1-ijn-10-6027: Synthetic route of the copolymer.Abbreviations: ε-CL, ε-caprolactone; PEI, polyethyleneimine; DCC, dicyclohexylcarbodiimide; NHS, N-hydroxy-succinimide; PEG-PCL-g-PEI, poly(ethylene glycol)-poly (ε-caprolactone)-g-polyethyleneimine.
Mentions: The triblock copolymer PCI was synthesized via a combination of ring-opening polymerization of ε-CL and an amidation reaction between the amine group of PEI and the carboxyl group of PCL, as outlined in Figure 1. The chemical structures of the copolymers were confirmed by 1H NMR and FTIR spectroscopy. In Figure 2, the 1H NMR spectra of the triblock copolymer PCI and the propolymer clearly show characteristic resonance peaks of PEG, PCL, and PEI. The sharp peak appearing at 3.64 ppm was attributed to the methylene protons in the PEG blocks. The typical signals of the methylene protons in the PCL blocks appeared at 1.32 ppm, 1.56 ppm, 2.31 ppm, and 4.06 ppm. The strong and broad absorption peaks that were observed at 2.5–2.9 ppm were assigned to the methane protons of PEI.27 The 1H NMR results showed that the PCI copolymer was successfully synthesized.

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