Design and characterization of Amoitone B-loaded nanostructured lipid carriers for controlled drug release

Abstract

Amoitone B, a novel compound chemically synthesized as the analogue of cytosporone B, has been proved to own superior affinity with Nur77 than its parent compound and exhibit notable anticancer activity. However, its application is seriously restricted due to the water-insolubility and short biological half-time. The aim of this study was to construct an effective delivery system for Amoitone B to realize sustained release, thus prolong drug circulation time in body and improve the bioavailability. Nanostructured lipid carriers (NLC) act as a new type of colloidal drug delivery system, which offer the advantages of improved drug loading and sustained release. Amoitone B-loaded NLC (AmB-NLC) containing glyceryl monostearate (GMS) and various amounts of medium chain triglycerides (MCT) were successfully prepared by emulsion-evaporation and low temperature-solidification technology with a particle size of about 200 nm and a zeta potential value of about À20 mV. The results of X-ray diffraction and DSC analysis showed amorphous crystalline state of Amoitone B in NLC. Furthermore, the drug entrapment efficacy (EE) was improved compared with solid lipid nanoparticles (SLN). The EE range was from 71.1% to 84.7%, enhanced with the increase of liquid lipid. In vitro drug release studies revealed biphasic drug release patterns with burst release initially and prolonged release afterwards and the release was accelerated with augment of liquid lipid. These results demonstrated that AmB-NLC could be a promising delivery system to control drug release and improve loading capacity, thus prolong drug action time in body and enhance the bioavailability.

Improved Stability of Polyglycerol Polyricinoleate‐Substituted Nanostructured Lipid Carrier Cholecalciferol Emulsions with Different Carrier Oils

“…In contrast to the control NLC (25.7 mV), all modified emulsions had a relatively high absolute value of zeta potential (39.5 to 67.8 mV) (Table ). The zeta potential obtained from the control NLC was comparable to that reported for NLCs produced using a similar method, which is about 20 mV (Luan et al., ). The low zeta potential value of the control may be a consequence of its large particle size.…”

“…The nonionic surfactant used in this case was PGPR, and primary destabilization phenomena, such as flocculation and coalescence, of the emulsions may have been prevented due to sufficiently small particle size. (Luan et al., ). However, in the case of GMS which existed in solid form at room temperature, this is attributed to form large particles by self‐crystallization different from the liquid type PGPR (Ghosh & Rousseau, ).…”

“…The Vitamin D 3 ‐loaded control NLC and the modified NLC emulsions with different carrier oil were prepared by emulsion evaporation at a high temperature (75 °C) and solidification at a low temperature (0 to 2 °C), similar to a previously described method with minor modifications (Luan et al., ). To prepare the oil phase of the control NLC, vitamin D 3 (100 mg), soybean lecithin (3 g), MCT (2.5 g), and GMS (4 g) were accurately measured and dissolved in hot ethanol (75 °C, 100 mL) in water bath.…”

Characterization and toxicity of citral incorporated with nanostructured lipid carrier

“…Being a small nanoparticle, NLC-Citral holds a potential in lowering the risk of non-specific liver uptake ( Seki et al, 2004 ) as well as increasing the actual distribution and bioavailability of the drug ( Fang et al, 2006 ). The incorporation of a water insoluble anticancer compound (Amoitone B) with NLC was reported to enhance its bioavailability ( Luan et al, 2013 ). Moreover, small nanoparticle with a diameter size of 50–60 nm resulted in high tumor uptake as well as sustained release of the drug in cancer biology studies ( Mitra et al, 2001 ; Sharma et al, 1996 ).…”

Advances in nanotechnology-based carrier systems for targeted delivery of bioactive drug molecules with special emphasis on immunotherapy in drug resistant tuberculosis – a critical review

“…The colloidal drug carrier system not only offers many advantages in the case of targeted drug delivery (Luan et al, 2013) but also increase bioavailability of some poorly soluble drugs and protection for sensitive active compounds (Wang & Xia, 2014). As nanostructured lipid carriers (NLCs) were developed in the midlines of the 1990s as an alternative carrier system to the existing traditional carriers (Kamble et al, 2012).…”