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Carbohydr Polym. 2018 Jan 1;179:135-144. doi: 10.1016/j.carbpol.2017.09.075. Epub 2017 Sep 25.

GABAB receptor ligand-directed trimethyl chitosan/tripolyphosphate nanoparticles and their pMDI formulation for survivin siRNA pulmonary delivery.

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Department of Pharmacy, China Pharmaceutical University, Nanjing 211198, PR China.
Department of Pharmacy, China Pharmaceutical University, Nanjing 211198, PR China. Electronic address:


The effect of gene silencing by survivin siRNA (siSurvivin) on the proliferation and apoptosis of lung tumor has been attracted more interest. GABAB receptor ligand-directed nanoparticles consisting of baclofen functionalized trimethyl chitosan (Bac-TMC) as polymeric carriers, tripolyphosphate (TPP) as ionic crosslinker, and siSurvivin as therapeutic genes, were designed to enhance the survivin gene silencing. GABAB receptor agonist baclofen (Bac) was initially introduced into TMC as a novel ligand. This Bac-TMC/TPP nanoparticles increased the uptake of survivin siRNA through the interaction with GABAB receptor, further resulted in efficient cell apoptosis and gene silencing. For siRNA-loaded nanoparticles pulmonary delivery, mannitol was utilized for it delivery into pressurized metered dose inhalers (pMDI). The fine particle fractions of this formulation was (45.39±2.99)% indicating the appropriate deep lung deposition. These results revealed that this pMDI formulation containing Bac-TMC/TPP nanoparticles would be a promising siRNA delivery system for lung cancer treatment.


Baclofen; Baclofen (PubChem CID: 2284); HFA-134a (PubChem CID: 13129); Mannitol (PubChem CID: 6251); Nanoparticles; Pressurized metered dose inhalers; Sodium tripolyphosphate (PubChem CID: 24455); Survivin siRNA; Trimethyl chitosan; Trimethyl chitosan (PubChem CID: none)

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