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Synthetic star shaped tetra-tailed biocompatible supramolecular amphiphile as an efficient nanocarrier for Amphotericin B.

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Title: Synthetic star shaped tetra-tailed biocompatible supramolecular amphiphile as an efficient nanocarrier for Amphotericin B.
Authors: Ali, Imdad1 (AUTHOR) imdadchem26@gmail.com, Burki, Samiullah2 (AUTHOR) sm_barki@hotmail.com, Rehman, Jawad ur1 (AUTHOR) jawadkhan4chem@gmail.com, Ullah, Shafi1 (AUTHOR) shafi_ullah34@yahoo.com, Javid, Ibrahim3 (AUTHOR) ibr_pharmacist@yahoo.com, Abdellattif, Magda H.4 (AUTHOR) m.hasan@tu.edu.sa, Shah, Muhammad Raza1 (AUTHOR) raza.shah@iccs.edu
Source: Chemistry & Physics of Lipids. Jan2023, Vol. 250, pN.PAG-N.PAG. 1p.
Subjects: Drug solubility, Polymersomes, Drug bioavailability, Surface charges, Amphotericin B, Zeta potential, Oral medication
Abstract: Macrocycle-based amphiphiles are capable of self-assembling into multidimensional nano-architecture with defined dimensions for various applications. Herein we report the synthesis, physio-chemical characterizations and oral drug delivery profiling of resorcinarene-based amphiphilic supramolecular macrocycle. The macrocycle was synthesized in two-step reaction and characterized using 1H NMR, Mass spectrometry and IR spectroscopic techniques. The synthesized macrocycle was assessed for vesicles formation, checked for biocompatibility and then Amphotericin B (Amp-B) was entrapped in macrocycle-based vesicles. The drug loaded vesicles were characterized for shape, size, homogeneity, drug entrapment, surface charge, in-vitro release profile and stability. Amp-B loaded macrocycle based vesicles were examined in rabbits for in-vivo bioavailability and compared with plan drug suspension. The synthesized macrocycle was non-toxic in normal mouse fibroblast cells, compatible with blood and safe in mice. The drug loaded macrocycle based vesicles appeared spherical with 279.4 nm size and − 12.2 mV zeta potential loading 85.45 % drug. The drug loaded vesicles storage stability for 30 days and gastric fluid stability for 1 h were it retained nearly 90 % drug at 30th day and 83.79 % drug at 1 h in gastric fluid. Oral bioavailability of Amp-B in rabbits was markedly enhanced when delivered in synthesized macrocycle based vesicles in comparison with plan drug suspension. Results of this study indicate that the synthesized star shaped tetra-tailed supramolecular amphiphile could be used as an efficient nanocarrier for enhancing oral bioavailability of drugs with solubility and bioavailability issues like Amp-B. [Display omitted] • Synthesis and characterization of Resorcinarene-based supramolecular macrocycle is presented. • The synthesized macrocycle was biocompatible, less toxic and able to encapsulate amphotericin B. • The drug-loaded macrocycle vesicles were 279.4 nm sized with − 12.2 mV zeta potential and 85.45 % drug loading. • The drug-loaded vesicle retained 90 % drug at 30th day and 83.79 % drug in 1 h gastric fluid storage. • Oral bioavailability of amphotericin B was enhanced when delivered in synthesized macrocycle based vesicles. [ABSTRACT FROM AUTHOR]
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Database: Engineering Source
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Abstract:Macrocycle-based amphiphiles are capable of self-assembling into multidimensional nano-architecture with defined dimensions for various applications. Herein we report the synthesis, physio-chemical characterizations and oral drug delivery profiling of resorcinarene-based amphiphilic supramolecular macrocycle. The macrocycle was synthesized in two-step reaction and characterized using 1H NMR, Mass spectrometry and IR spectroscopic techniques. The synthesized macrocycle was assessed for vesicles formation, checked for biocompatibility and then Amphotericin B (Amp-B) was entrapped in macrocycle-based vesicles. The drug loaded vesicles were characterized for shape, size, homogeneity, drug entrapment, surface charge, in-vitro release profile and stability. Amp-B loaded macrocycle based vesicles were examined in rabbits for in-vivo bioavailability and compared with plan drug suspension. The synthesized macrocycle was non-toxic in normal mouse fibroblast cells, compatible with blood and safe in mice. The drug loaded macrocycle based vesicles appeared spherical with 279.4 nm size and − 12.2 mV zeta potential loading 85.45 % drug. The drug loaded vesicles storage stability for 30 days and gastric fluid stability for 1 h were it retained nearly 90 % drug at 30th day and 83.79 % drug at 1 h in gastric fluid. Oral bioavailability of Amp-B in rabbits was markedly enhanced when delivered in synthesized macrocycle based vesicles in comparison with plan drug suspension. Results of this study indicate that the synthesized star shaped tetra-tailed supramolecular amphiphile could be used as an efficient nanocarrier for enhancing oral bioavailability of drugs with solubility and bioavailability issues like Amp-B. [Display omitted] • Synthesis and characterization of Resorcinarene-based supramolecular macrocycle is presented. • The synthesized macrocycle was biocompatible, less toxic and able to encapsulate amphotericin B. • The drug-loaded macrocycle vesicles were 279.4 nm sized with − 12.2 mV zeta potential and 85.45 % drug loading. • The drug-loaded vesicle retained 90 % drug at 30th day and 83.79 % drug in 1 h gastric fluid storage. • Oral bioavailability of amphotericin B was enhanced when delivered in synthesized macrocycle based vesicles. [ABSTRACT FROM AUTHOR]
ISSN:00093084
DOI:10.1016/j.chemphyslip.2022.105257