Advancing the Therapeutic Efficacy of Bioactive Molecules by Delivery Vehicle Platforms

Abstract

: Drugs have to overcome numerous barriers to reach their desired therapeutic targets. In several cases drugs, especially the highly lipophilic molecules, suffer from low solubility and bioavailability and therefore their desired targeting is hampered. In addition, undesired metabolic products might be produced or off-targets could be recognized. Along these lines, nanopharmacology has provided new technological platforms, to overcome these boundaries. Specifically, numerous vehicle platforms such as cyclodextrins and calixarenes have been widely utilized to host lipophilic drugs such as antagonists of the angiotensin II AT1 receptor (AT1R), as well as quercetin and silibinin. The encapsulation of these drugs in supramolecules or other systems refines their solubility and metabolic stability, increases their selectivity and therefore decreases their effective dose and improves the therapeutic index. In this minireview we report on the formulations of Silibinin and AT1R antagonist candesartan in a 2-HP-β-cyclodextrin host molecule, which displayed enhanced cytotoxicity and increased silibinin’s and candesartan’s stability, respectively. Moreover we describe the encapsulation of quercetin in gold nanoparticles bearing a calixarene supramolecular host. Also the encapsulation of temozolomide in a calixarene nanocapsule has been described. Finally, we report on the activity enhancement that has been achieved upon using these formulations as well as the analytical and computational methods we used to characterize these formulations and explore the molecular interactions between the host and quest molecules.

Computational Methods for the Interaction between Cyclodextrins and Natural Compounds: Technology, Benefits, Limitations, and Trends

“…However, the guest molecules are not only limited to natural compounds in practical applications but are also small chemical molecules or drugs. These related studies and discussion are beyond the scope of this review and can be found in related reports. , …”

“…These related studies and discussion are beyond the scope of this review and can be found in related reports. 128,129 For the selection and application of computational methods in CD−guest interaction studies, we would like to provide the following suggestions:…”

Application of Biomedical Microspheres in Wound Healing

“…Therefore, it is considered to be a promising dressing that can better repair the skin. Drugs commonly encapsulated in the spheroid sustained release system and used for wound healing include antimicrobials, growth factors, nucleic acids, and other bioactive molecules [ 149 ]. For example, Juan Liu et al prepared the gelatin microsphere (GM) loaded curcumin (Cur) nanoparticles (CNPs), and they were loaded into thermos-sensitive hydrogel.…”

Chimonanthus salicifolius attenuated vascular remodeling by alleviating endoplasmic reticulum stress in spontaneously hypertensive rats

“…6 Phytochemical studies on CS reveal that flavonoids are abundant in its aqueous extract, such as rutin, kaempferol and quercetin. 7 Several compounds in CS attenuate vascular remodeling under hypertension [8][9][10] and could regulate the renin angiotensin system as angiotensin receptor blockers, such as quercetin, 11 luteolin 12 and catechin. 13 However, due to the limited geographical distribution of this plant, the phytochemical and pharmacological study of CS is seldom reported.…”