Amphotericin B Loaded Chitosan Nanoparticles: Implication of Bile Salt Stabilization on Gastrointestinal Stability, Permeability and Oral Bioavailability
Through current investigation, we presented a lucrative way to formulate amphotericin B loaded bile salt stabilized carbohydrate polymer i.e. chitosan nanoparticles (NPs) for enhancing gastrointestinal stability of NPs thereby increasing the oral bioavailability of the drug. NPs were prepared using ionic gelation method, and stabilized using bile salt to provide gastric pH stability to chitosan NPs. NPs were optimized on different parameters such as particle size, encapsulation efficiency and estimated for their in vitro and in vivo performance. Developed NPs presented a higher stability in gastrointestinal milieu, reduced haemolytic toxicity and significantly higher uptake in Caco-2 cell lines followed by increased bioavailability as compared to naive drug, marketed formulation i.e. Fungizone® and uncoated chitosan NPs. Biochemical parameters and histology further substantiated the lower toxicity. In nutshell, the present research explored the bioadhesive and higher uptake potential of cationic carbohydrate polymer at the same time along with bile salts for stabilization of NPs in gastric milieu.
KEY WORDSamphotericin B chitosan bile salts oral bioavailability GI stability nephrotoxicity
- AmB-CSCA NPs
AmB loaded bile salt stabilized chitosan nanoparticles
Analysis of variance
Area under the curve
Blood urea nitrogen
High-performance liquid chromatography
Red blood cells
Scanning electron microscopy
Simulated gastric fluid
Simulated intestinal fluid
Sodium lauryl sulphate
Transmission electron microscope
The authors are thankful to Director, NIPER for providing the necessary infrastructure and facilities and Department of Science & Technology (DST), Government of India, New Delhi, and financial support. Rajan Swami is grateful to Science and Engineering Research Board (SERB), DST, GOI, New Delhi, for providing research fellowship. Varun Kushwah is appreciative to CSIR, GOI, New Delhi, for providing fellowships.
Compliance with Ethical Standards
Conflict of Interest
The authors report no financial interest that might pose a potential, perceived, or real conflict.
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