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Development and Characterization of PCL Electrospun Membrane-Coated Bletilla striata Polysaccharide-Based Gastroretentive Drug Delivery System

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Abstract

The purpose of this study was to investigate the potential of Bletilla striata polysaccharide (BSP, a natural glucomannan material) for the development of a gastroretentive drug delivery system for the first time. Novel BSP-based porous wafer was prepared for levofloxacin hydrochloride (LFH) delivery by combining floating, swelling, and mucoadhesion mechanisms. The influences of BSP and ethyl cellulose (EC) on drug release and mucoadhesive strength were studied by 32 factorial design. The optimized matrix was coated with polycaprolactone (PCL) electrospun membrane by electrospinning and heat treatment technology. The optimized formula (F6, coated) exhibited Q4 h of 41.20 ± 1.90%, Q8 h of 76.49 ± 1.69%, and mucoadhesive strength of 86.11 ± 1.33 gf, and its drug release profile most closely resembled the Korsmeyer–Peppas model with anomalous diffusion driving mechanism. F6 (coated) also presented excellent buoyancy, preferred swelling characteristic due to the porous structure formed by freeze-drying. Meanwhile, the internal morphology, physical state, drug–excipient compatibility, and thermal behavior were recorded. The negligible cytotoxicity of F6 (coated) was observed in human gastric epithelial cell cultures. In the in vitro antimicrobial experiment, the prepared wafer exhibited obvious bacterial inhibition zone, and due to its longer gastric retention, the wafer also performed a more effective Helicobacter pylori clearance than free LFH in vivo.

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Abbreviations

BSP:

Bletilla striata polysaccharide

DSC:

Differential scanning calorimeter

EC:

Ethyl cellulose

FTIR:

Fourier transform infrared spectroscopy

GES-1:

Human gastric mucosal epithelial cells

GRDDS:

Gastroretentive drug delivery system

H. pylori :

Helicobacter pylori

LFH:

Levofloxacin hydrochloride

PCL:

Polycaprolactone

Q 4 h :

Cumulative release of the drug at 4 h

Q 8 h :

Cumulative release of the drug at 8 h

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Author information

Correspondence to Yan Qu.

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Ethical Approval

All the animal experiments were approved and supervised/conducted by the Chengdu University of Traditional Chinese Medicine Ethics Committee of Care and Use of Laboratory Animals, and the animals were house and handled according to the University Unit for Laboratory Animal Medicine guidelines.

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The authors declare that they have no conflicts of interest.

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Li, Z., Zeng, R., Yang, L. et al. Development and Characterization of PCL Electrospun Membrane-Coated Bletilla striata Polysaccharide-Based Gastroretentive Drug Delivery System. AAPS PharmSciTech 21, 66 (2020). https://doi.org/10.1208/s12249-019-1607-5

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KEY WORDS

  • floating
  • gastroretentive
  • Bletilla striata polysaccharide
  • controlled release
  • Helicobacter pylori