Ion-pair amphiphiles (IPAs) are neoteric pseudo-double-tailed compounds with potential as a novel substitute of phospholipid. IPA, synthesized by stoichiometric/equimolar mixing of aqueous solution of hexadecyltrimethylammonium bromide (HTMAB) and sodium dodecyl sulfate (SDS), was used as a potential substituent of naturally occurring phospholipid, soylecithin (SLC). Vesicles were prepared using SLC and IPA in different ratios along with cholesterol. The impact of IPA on SLC was examined by way of surface pressure (π)-area (A) measurements. Associated thermodynamic parameters were evaluated; interfacial miscibility between the components was found to depend on SLC/IPA ratio. Solution behavior of the bilayers, in the form of vesicles, was investigated by monitoring the hydrodynamic diameter, zeta potential, and polydispersity index over a period of 100 days. Size and morphology of the vesicles were also investigated by electron microscopic studies. Systems comprising 20 and 40 mol % IPA exhibited anomalous behavior. Thermal behavior of the vesicles, as scrutinized by differential scanning calorimetry, was correlated with the hydrocarbon chain as well as the headgroup packing. Entrapment efficiency (EE) of the vesicles toward the cationic dye methylene blue (MB) was also evaluated. Vesicles were smart enough to entrap the dye, and the efficiency was found to vary with IPA concentration. EE was found to be well above 80% for some stable dispersions. Such formulations thus could be considered to have potential as novel drug delivery systems.
This study aimed to investigate the effect of hydrocarbon chain length of nonionic surfactants, Tween 40 and Tween 60, on the physicochemical properties of nanostructured lipid carriers (NLCs). Two local anaesthetics, lidocaine (LIDO) and procaine hydrochloride (PRO$HCl), were incorporated in the NLCs.NLC formulations were prepared using sorbitantristearate (Span 65), soy lecithin (SLC) and stearic acid (SA) in a 2 : 2 : 1 mole ratio employing the hot homogenization technique. The systems were characterized by combined dynamic light scattering (DLS), transmission electron microscopy (TEM), differential scanning calorimetry (DSC) and spectroscopic studies. The formulations were found to be stable up to 60 days when kept at 4 C. NLCs stabilized by Tween 60 were superior to the corresponding Tween 40 based formulations. A spherical morphology with smooth surfaces was evidenced by TEM measurements. DSC and polarity studies indicated that LIDO altered the crystallinity of the lipid matrices as it could insert into the core of the NLC. Entrapment efficiency (EE) and loading content (LC) studies revealed that Tween 60 stabilized NLCs have better drug loading capability than the Tween 40 based formulation. Controlled and prolonged drug release was experienced by Tween 60 stabilized drug loaded NLCs as studied by in vitro release kinetics. The developed NLCs could thus be considered to have prospects as novel drug carriers for controlled/sustained release to improve the time duration of anaesthesia, especially for topical application.
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.
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