Polyhydroxyethylaspartamide-based micelles for ocular drug delivery

Civiale, C.; Licciardi, Mariano; Cavallaro, Gennara; Giammona, Gaetano; Mazzone, Maria Grazia

doi:10.1016/j.ijpharm.2009.05.028

Cited by 107 publications

(53 citation statements)

References 29 publications

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“…[112][113][114][115][116][117][118][119] In a recently published review Cholkar and Mitra have discussed in detail about methods for nanomicelle preparation and their applications in ocular drug delivery. 94 Recently, Pepic et al attempted to deliver the dexamethasone-encapsulated Pluronic/chitosan micellar system.…”

Section: Formulation Approaches For Anterior Chamber Deliverymentioning

confidence: 99%

Novel Strategies for Anterior Segment Ocular Drug Delivery

Cholkar

Patel

Vadlapudi

et al. 2013

Journal of Ocular Pharmacology and Therapeutics

148

107

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Research advancements in pharmaceutical sciences have led to the development of new strategies in drug delivery to anterior segment. Designing a new delivery system that can efficiently target the diseased anterior ocular tissue, generate high drug levels, and maintain prolonged and effective concentrations with no or minimal side effects is the major focus of current research. Drug delivery by traditional method of administration via topical dosing is impeded by ocular static and dynamic barriers. Various products have been introduced into the market that prolong drug retention in the precorneal pocket and to improve bioavailability. However, there is a need of a delivery system that can provide controlled release to treat chronic ocular diseases with a reduced dosing frequency without causing any visual disturbances. This review provides an overview of anterior ocular barriers along with strategies to overcome these ocular barriers and deliver therapeutic agents to the affected anterior ocular tissue with a special emphasis on nanotechnology-based drug delivery approaches.

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Section: Formulation Approaches For Anterior Chamber Deliverymentioning

confidence: 99%

Novel Strategies for Anterior Segment Ocular Drug Delivery

Cholkar

Patel

Vadlapudi

et al. 2013

Journal of Ocular Pharmacology and Therapeutics

148

107

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“…19 Topical formulations of drug-loaded polymeric micelles hold significant promise for ophthalmic drug delivery. 20,21 The particle size and potential of polymeric micelles are the two main factors that influence their ophthalmic application. 22 Small, positively charged nanoparticles may be useful as penetration enhancers for ocular drug delivery.…”

Section: Introductionmentioning

confidence: 99%

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

Li¹,

Li²,

Zhou³

et al. 2015

IJN

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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.

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“…For example, Civiale et al (2009) used the nanomicelle carrying dexamethasone to anterior eye segment by PEHAC (16). In vivo, Scientists took samples from the aqueous humor of rabbits to study the concentration-time curve of dexamethasone.…”

Section: Nanomicelles In Drug Deliverymentioning

confidence: 99%