Influence of Lipid Core Material on Physicochemical Characteristics of an Ursolic Acid-Loaded Nanostructured Lipid Carrier: An Attempt To Enhance Anticancer Activity

Abstract

The impact of saturation and unsaturation in the fatty acyl hydrocarbon chain on the physicochemical properties of nanostructured lipid carriers (NLCs) was investigated to develop novel delivery systems loaded with an anticancer drug, ursolic acid (UA). Aqueous NLC dispersions were prepared by a high-pressure homogenization-ultrasonication technique with Tween 80 as a stabilizer. Mutual miscibility of the components at the air-water interface was assessed by surface pressure-area measurements, where attractive interactions were recorded between the lipid mixtures and UA, irrespective of the extent of saturation or unsaturation in fatty acyl chains. NLCs were characterized by combined dynamic light scattering, transmission electron microscopy (TEM), atomic force microscopy (AFM), differential scanning calorimetry, drug encapsulation efficiency, drug payload, in vitro drug release, and in vitro cytotoxicity studies. The saturated lipid-based NLCs were larger than unsaturated lipids. TEM and AFM images revealed the spherical and smooth surface morphology of NLCs. The encapsulation efficiency and drug payload were higher for unsaturated lipid blends. In vitro release studies indicate that the nature of the lipid matrix affects both the rate and release pattern. All UA-loaded formulations exhibited superior anticancer activity compared to that of free UA against human leukemic cell line K562 and melanoma cell line B16.

Polyester-Based Dendrimer Nanoparticles Combined with Etoposide Have an Improved Cytotoxic and Pro-Oxidant Effect on Human Neuroblastoma Cells

“…Nanoparticles are extensively inspected to prepare multifunctional smart materials [26][27][28][29][30] and are widely employed in various biomedical applications [31][32][33][34][35][36][37][38][39][40][41][42][43][44][45][46][47][48][49].…”

Ursolic acid: Pharmacokinetics process in vitro and in vivo, a mini review

“…For these reasons, some new approaches have been introduced to enhance the biopharmaceutical properties of this compound of UA, particularly drug delivery technologies. At present, several UA delivery systems have been used successfully, such as nano‐emulsions, mesoporous silica nanoparticles, solid lipid nanoparticles, liposomes, niossomal gels, and solid dispersions . These preparations will change pharmacokinetic features of UA.…”

Physicochemical Characterization of Chrysin‐Derivative‐Loaded Nanostructured Lipid Carriers with Special Reference to Anticancer Activity

“…Because of the higher DL capacity, sustained release of the loaded drug, and the reduced size of LCD‐loaded NLC, cytotoxicity was effectively enhanced. The reduced size of the formulation enhanced the cell penetration of the LCD‐loaded NLC and the enhanced hydrophobicity of the LCD effectively, increasing the cellular uptake (Nahak et al, ). Further studies with different cancer cell lines and in vivo evaluation of the anticancer efficacy of CHR and LCD‐loaded NLC formulations are warranted.…”