<p>Preparation, intestinal segment stability, and mucoadhesion properties of novel thymopentin-loaded chitosan derivatives coated with poly (n-butyl) cyanoacrylate nanoparticles</p>

Abstract

Background: In order to develop a promising carrier for the oral delivery of proteins and peptide drugs, a novel bioadhesive nanocarrier of chitosan (CTS) derivatives coated with poly (n-butyl) cyanoacrylate nanoparticles (PBCA-NPs) was prepared in this study. Methods: Three different thymopentin (TP5)-loaded nanoparticles were prepared in the present study. TP5-PBCA-NPs were developed by modifying an emulsion polymerization method, and CTS and chitosan-glutathione (CG) derivative-coated PBCA nanoparticles were obtained from the electrostatic interactions between CTS or CG with negatively charged PBCA nanoparticles. Results: The particle sizes of TP5-PBCA-NPs, TP5-CTS-PBCA-NPs, and TP5-CG-PBCA-NPs were 212.3±6.9, 274.6±8.2, and 310.4±7.5 nm, respectively, while the respective zeta potentials were-22.6±0.76, 23.3±1.2, and 34.6±1.6 mV with encapsulation efficiencies of 79.37%±2.15%, 74.21%±2.13%, and 72.65%±1.48%, respectively. An everted intestinal ring method indicated that drug stability was remarkably improved after incorporation into the nanoparticles, especially the CG-coated nanoparticles. The mucus layer retention rates for CTS-and CG-coated nanoparticles were 1.43 and 1.83 times that of the uncoated nanoparticles, respectively, using ex vivo mucosa. The in vivo mucoadhesion study illustrated that the transfer of uncoated PBCA-NPs from the stomach to the intestine was faster than that of CTS-PBCA-NPs and CG-PBCA-NPs, while the CG-PBCA-NPs presented the best intestinal retentive characteristic. Conclusion: In summary, this study demonstrated the feasibility and benefit of orally delivering peptide drugs using novel CTS derivative-coated nanoparticles with optimal stability and bioadhesive properties.

An Integrative in silico Drug Repurposing Approach for Identification of Potential Inhibitors of SARS‐CoV‐2 Main Protease

“…However, all of these drugs show limited oral absorption [67][68][69][70][71][72] due to poor biopharmaceutical or pharmacokinetic properties. Namely, QSPR predictions indicate that all six drugs are substrates for P-gp efflux transporters, in addition to low passive permeability of ritonavir, dipyridamole and thymopentin, and first pass metabolism of montelukast, ritonavir, lopinavir, dipyridamole and telmisartan.…”

An Integrative in Silico Drug Repurposing Approach for Identification of Potential Inhibitors of SARS-CoV-2 Main Protease

“…However, all of these drugs show limited oral absorption [67][68][69][70][71][72] into kidneys and lungs. 72,74 These data support the value of in silico simulation results, and…”

Quercetin and Its Nano-Formulations for Brain Tumor Therapy—Current Developments and Future Perspectives for Paediatric Studies

“…In recent years, poly(n-butylcyanoacrylate) nano-particles (PBCA NP) have received considerable interest due to PBCA ability to overcome the limitation of other colloidal carriers [ 111 ]. PBCA has been widely investigated for targeted drug delivery due to its properties such as biodegradation, biocompatibility, bioadhesion and low toxicity [ 112 , 113 ]. The most remarkable findings of PBCA NP coated with polysorbate-80 (P-80) on their surfaces showed effectiveness in brain delivery since the particles entrap the compounds and prevent rapid elimination thus leading to enhancement through blood–brain penetration [ 114 ].…”