4.7 Article

N-acetylcysteine functionalized chitosan oligosaccharide-palmitic acid conjugate enhances ophthalmic delivery of flurbiprofen and its mechanisms

Journal

CARBOHYDRATE POLYMERS
Volume 291, Issue -, Pages -

Publisher

ELSEVIER SCI LTD
DOI: 10.1016/j.carbpol.2022.119552

Keywords

N -acetylcysteine; Chitosan oligosaccharide; Ophthalmic delivery; Flurbiprofen

Funding

  1. National Natural Science Foundation of China [81703717]
  2. National College Student Innovation and Entrepreneurship Training Program [201910440029]
  3. Shandong Provincial Natural Science Foundation [ZR2014HQ069]
  4. Shandong Province Taishan Scholar Project [ts201712067, tsqn201909143]

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An N-acetylcysteine functionalized chitosan oligosaccharide-palmitic acid conjugate (NAC-COS-PA) was synthesized for enhanced transocular drug delivery. The conjugate exhibited good biocompatibility and increased drug permeation. In vivo studies showed that NAC-COS-PA-FB had superior anti-inflammatory efficacy compared to other nanomicelles and solution.
An N-acetylcysteine functionalized chitosan oligosaccharide-palmitic acid conjugate (NAC-COS-PA) with bioadhesive and permeation promoting properties was synthesized to enhance transocular drug delivery. Flurbiprofen (FB) loaded self-assembled NAC-COS-PA nanomicelles (NAC-COS-PA-FB) were prepared and the drug loading was 7.35 +/- 0.32%. Human immortalized corneal epithelial (HCE-T) cell cytotoxicity and hen's egg testchorioallantoic membrane assays confirmed that the conjugate had good biocompatibility. The transportation efficiency of coumarin-6 (C6) loaded nanomicelles in the HCE-T cell monolayer was approximately 1.97 times higher than that of free C6. Decreased intracellular Ca2+ concentration and cell membrane potential, increased cell membrane fluidity, and reversible changes in the F-actin cytoskeleton are presumed to be responsible for the enhanced drug permeation. NAC-COS-PA exhibited strong binding capacity with mucin and rabbit eyeball. In vivo pharmacokinetics indicated that the area under the curve (AUC0-6 h) and the maximum concentration (Cmax) of NAC-COS-PA-FB were approximately 1.92 and 2.44 times that of the FB solution, respectively. NACCOS-PA-FB demonstrated the best in vivo anti-inflammatory efficacy compared to unfunctionalized nanomicelles (COS-PA-FB) and FB solution. Consequently, NAC-COS-PA appears to be a promising bioadhesive carrier for ophthalmic delivery.

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