PLGA-PEG-Maleimide used for developed to improve ocular delivery mechanisms
PolySciTech
division of Akina, Inc. (www.polyscitech.com)
provides a wide variety of active end-capped PLGA-PEG precursors for
development of targeted nanoparticles. Recently, PLGA-PEG-Maleimide was used to
generate peptide conjugated nanoparticles for improved ocular delivery. Read more:
Vasconcelos, Aimee, Estefania Vega, Yolanda Pérez, María J. Gómara, María Luisa
García, and Isabel Haro. "Conjugation of cell-penetrating peptides with
poly (lactic-co-glycolic acid)-polyethylene glycol nanoparticles improves
ocular drug delivery." International journal of nanomedicine 10 (2015):
609. Full-text http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4315550/
“Abstract:
In this work, a peptide for ocular delivery (POD) and human immunodeficiency
virus transactivator were conjugated with biodegradable poly(lactic-co-glycolic
acid) (PGLA)–polyethylene glycol (PEG)-nanoparticles (NPs) in an attempt to improve
ocular drug bioavailability. The NPs were prepared by the solvent displacement
method following two different pathways. One involved preparation of PLGA NPs
followed by PEG and peptide conjugation (PLGA-NPs-PEG-peptide); the other
involved self-assembly of PLGA-PEG and the PLGA-PEG-peptide copolymer followed
by NP formulation. The conjugation of the PEG and the peptide was confirmed by
a colorimetric test and proton nuclear magnetic resonance spectroscopy.
Flurbiprofen was used as an example of an anti-inflammatory drug. The
physicochemical properties of the resulting NPs (morphology, in vitro release,
cell viability, and ocular tolerance) were studied. In vivo anti-inflammatory
efficacy was assessed in rabbit eyes after topical instillation of sodium arachidonate.
Of the formulations developed, the PLGA-PEG-POD NPs were the smaller particles
and exhibited greater entrapment efficiency and more sustained release. The
positive charge on the surface of these NPs, due to the conjugation with the
positively charged peptide, facilitated penetration into the corneal
epithelium, resulting in more effective prevention of ocular inflammation. The
in vitro toxicity of the NPs developed was very low; no ocular irritation in
vitro (hen’s egg test–chorioallantoic membrane assay) or in vivo (Draize test)
was detected. Taken together, these data demonstrate that PLGA-PEG-POD NPs are
promising vehicles for ocular drug delivery. Keywords: peptide for ocular
delivery, flurbiprofen, controlled release, ocular tolerance, anti-inflammatory”
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