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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

FTIR spectra of the diblock intermediates PEG-PCL-COOH (A) and PCI (B).Abbreviations: PEG, poly(ethylene glycol); PCL, poly(ε-caprolactone); PCI, poly (ethylene glycol)-poly(ε-caprolactone)-g-polyethyleneimine; FTIR, Fourier transform infrared spectroscopy.
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f3-ijn-10-6027: FTIR spectra of the diblock intermediates PEG-PCL-COOH (A) and PCI (B).Abbreviations: PEG, poly(ethylene glycol); PCL, poly(ε-caprolactone); PCI, poly (ethylene glycol)-poly(ε-caprolactone)-g-polyethyleneimine; FTIR, Fourier transform infrared spectroscopy.

Mentions: Figure 3 shows the FTIR spectra of the diblock intermediates and final triblock PCI copolymer. The PEG and PCL blocks were characterized by prominent absorptions at ~1,190 cm−1 (s, νC–O) and 1,726 cm−1 (s, νC=O), respectively. Obviously, both PEG and PCL blocks are present in both the intermediate prepolymers and the final copolymer. The two new and strong absorption peaks that appeared in the spectrum of the triblock copolymer at ~1,644 cm−1 and 1,562 cm−1 were attributed to amide linkages (s, νamide, C=O). In addition, the PCI copolymer showed a strong and broad characteristic absorption of amines at ~3,300 cm−1 (s, νN–H). The FTIR results are consistent with the expected structures of the intermediate prepolymers and the final copolymers.


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)

FTIR spectra of the diblock intermediates PEG-PCL-COOH (A) and PCI (B).Abbreviations: PEG, poly(ethylene glycol); PCL, poly(ε-caprolactone); PCI, poly (ethylene glycol)-poly(ε-caprolactone)-g-polyethyleneimine; FTIR, Fourier transform infrared spectroscopy.
© Copyright Policy
Related In: Results  -  Collection

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

f3-ijn-10-6027: FTIR spectra of the diblock intermediates PEG-PCL-COOH (A) and PCI (B).Abbreviations: PEG, poly(ethylene glycol); PCL, poly(ε-caprolactone); PCI, poly (ethylene glycol)-poly(ε-caprolactone)-g-polyethyleneimine; FTIR, Fourier transform infrared spectroscopy.
Mentions: Figure 3 shows the FTIR spectra of the diblock intermediates and final triblock PCI copolymer. The PEG and PCL blocks were characterized by prominent absorptions at ~1,190 cm−1 (s, νC–O) and 1,726 cm−1 (s, νC=O), respectively. Obviously, both PEG and PCL blocks are present in both the intermediate prepolymers and the final copolymer. The two new and strong absorption peaks that appeared in the spectrum of the triblock copolymer at ~1,644 cm−1 and 1,562 cm−1 were attributed to amide linkages (s, νamide, C=O). In addition, the PCI copolymer showed a strong and broad characteristic absorption of amines at ~3,300 cm−1 (s, νN–H). The FTIR results are consistent with the expected structures of the intermediate prepolymers and the final copolymers.

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