PolySciTech
division of Akina, Inc. (www.polyscitech.com)
provides a wide array of biodegradable block copolymers including mPEG-PLA and
Mal-PEG-PLA. Recently researchers used these types of polymers to generate RGD
(arginine-glycine-aspartic acid a general binding domain for many cell types)
decorated nanoparticles for delivery of minocycline to bacteria for treatment
of periodontal infection. Read more: Yao, Wenxin, Peicheng Xu, Jingjing Zhao,
Li Ling, Xiaoxia Li, Bo Zhang, Nengneng Cheng, and Zhiqing Pang. "RGD
functionalized polymeric nanoparticles targeting periodontitis epithelial cells
for the enhanced treatment of periodontitis in dogs." Journal of colloid
and interface science 458 (2015): 14-21. (http://www.sciencedirect.com/science/article/pii/S0021979715300515)
“Abstract: Long
term retention of antimicrobials with effective drug concentration in gingival
crevicular fluid (GCF) is of vital importance for the treatment of chronic
periodontitis. In this study, a novel epithelial cell-targeting nanoparticle
drug delivery system by conjugating minocycline-loaded poly(ethylene
glycol)–poly(lactic acid) (PEG–PLA) nanoparticles (NP-MIN) with RGD peptide
were developed and administrated locally for targeting periodontitis epithelial
cells and enhancing the treatment of periodontitis in dogs. Biodegradable
NP-MIN was made with an emulsion/solvent evaporation technique. RGD peptide was
conjugated to the surface of nanoparticles via Maleimide group reaction with hydrosulfide
in RGD peptide (RGD-NP-MIN). Transmission electron microscopy examination and
dynamic light scattering results revealed that RGD-NP-MIN had a sphere shape,
with a mean diameter around 106 nm. In vitro release of minocycline from
RGD-NP-MIN showed that RGD modification did not change the remarkable sustained
releasing characteristic of NP-MIN. To elucidate the interaction of RGD-NP and
epithelial cells, RGD-NP binding, uptake and cellular internalization
mechanisms by calu-3 cells were investigated. It was shown RGD modification
significantly enhanced nanoparticles binding and uptake by Calu-3 cells, and
RGD-NP uptake was an energy-dependent process through receptor-mediated
endocytosis. Both clathrin-associated endocytosis and caveolae-dependent
endocytosis pathway were involved in the RGD-NP uptake, and the intracellular
transport of RGD-NP was related to lysosome and Golgi apparatus. Finally, in
vivo pharmacokinetics of minocycline in the periodontal pockets and
anti-periodontitis effects of RGD-NP-MIN on periodontitis-bearing dogs were
evaluated. After local administration of RGD-NP-MIN, minocycline concentration
in gingival crevicular fluid decreased slowly and maintained an effective drug
concentration for a longer time than that of NP-MIN. Anti-periodontitis effects
demonstrated that RGD-NP-MIN could significantly decrease symptoms of
periodontitis, which was better than any other control group. These findings
suggested that these epithelial cell-targeting nanoparticles offered a novel
and effective local delivery system for the treatment of periodontitis. Keywords:
RGD peptide; Polymeric nanoparticles; Targeting periodontitis epithelial cells;
Minocycline; Local delivery”
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