Post-synthesis nanostructuration of BSA-Capsaicin nanoparticles generated by sucrose excipient

Abstract

In the pharmaceutical industry nano-hydrocolloid systems frequently coalesce or present nanoparticle aggregation after a long storage periods. Besides, the lyophilization process used to dry nanoparticles (NPs) produces loss of their original properties after dispersion. In this work we evaluated the effect on morphology and physicochemical properties of different protective excipients during drying of bovine serum albumin (BSA) NPs loaded with different concentrations of capsaicin. Capsaicin concentrations of 0, 812, 1625, 2437, and 3250 µg mL−1 were used; subsequently, NPs were dried with deionized water (DW), NaCl (DN), sucrose (DS), and not dried (ND). We found that ND, DW, and DN treatments showed a negative effect on the NPs properties; while, DS reduced the aggregation and produced the formation of isolated nanoparticles at higher concentrations of capsaicin (3250 µg mL−1), improving their circular shape, morphometrical parameters, and ζ-potential. The stability of the BSA-capsaicin NPs was associated to complex capsaicin/amino acid/water, in which GLY/GLN, ALA/HIS, ARG, THR, TYR, and Iso/CYS amino acids are involved in the restructuration of capsaicin molecules into the surface of nanoparticles during the drying process. The secondary nanostructuration in the post-synthesis stage can improve the molecular stability of the particles and the capacity of entrapping hydrophobic drugs, like capsaicin.

Evaluation of Antidepressant Activity of Capsaicin Nanoemulsion in Nicotine Withdrawal-Induced Depression in Mice

“…Numerous investigations have represented nanoemulsion as a potential drug delivery carrier for phytochemicals and bioactive compounds, due to their tremendous advantages in solubility enhancement, spontaneous emulsification, and thermodynamic and kinetic stability over ordinary emulsions [10][11][12][13][14]. Various nanomaterials-based drug delivery carriers, such as nanoliposomes [15]; polymeric micelles [16]; solid lipid nanoparticles [17][18][19]; polymeric nanoparticles [20][21][22][23]; nanostructured lipid carriers [17,24,25]; and silver nanoparticles [26] of CAP have been studied in literature for the enhancement of CAP's drug delivery potential, skin penetration, therapeutic potential, and pharmacokinetic profile. A nanoemulsion formulation of CAP has also been studied to enhance its skin penetration potential [27].…”

Enhanced Bioavailability of Dihydrotanshinone I–Bovine Serum Albumin Nanoparticles for Stroke Therapy

“…Besides, owing to its low molecular weight, this small-molecule drug has a short blood half-life and it is difficult to guarantee the local concentration of the drug after intravenous administration (Gao Abbreviations: BBB, Blood brain barrier; BSA, Bovine serum albumin; CAT, Catalase; CBF, Cerebral blood flow; DHT, Dihydrotanshinone I; DHT-BSA NPs, DHT-BSA nanoparticles; GSH, Glutathione; MCAO/R, Middle cerebral artery occlusion/reperfusion; MDA, Malondialdehyde; OCT, Optical correlation tomography; SOD, Superoxide dismutase. Carriles et al, 2021). Even worse, the presence of the blood-brain barrier (BBB) further impairs the therapeutic effect of this agent after stroke (Sadeghi et al, 2014).…”

“…However, the aqueous solubility and biocompatibility of this molecule are rather low, which largely hampers its biological applications ( D’Agostino et al, 2015 ; Ye et al, 2012 ; Xu et al, 2020 ). Besides, owing to its low molecular weight, this small-molecule drug has a short blood half-life and it is difficult to guarantee the local concentration of the drug after intravenous administration ( Gao et al, 2018 ; Carriles et al, 2021 ). Even worse, the presence of the blood–brain barrier (BBB) further impairs the therapeutic effect of this agent after stroke ( Sadeghi et al, 2014 ).…”