Box–Behnken study design for optimization of bicalutamide-loaded nanostructured lipid carrier: stability assessment

Abstract

Bicalutamide (BCM) is an anti-androgen drug used to treat prostate cancer. In this study, nanostructured lipid carriers (NLCs) were chosen as a carrier for delivery of BCM using Box-Behnken (BB) design for optimizing various quality attributes such as particle size and entrapment efficiency which is very critical for efficient drug delivery and high therapeutic efficacy. Stability of formulated NLCs was assessed with respect to storage stability, pH stability, hemolysis, protein stability, serum protein stability and accelerated stability. Hot high-pressure homogenizer was utilized for formulation of BCM-loaded NLCs. In BB response surface methodology, total lipid, % liquid lipid and % soya lecithin was selected as independent variable and particle size and %EE as dependent variables. Scanning electron microscopy (SEM) was done for morphological study of NLCs. Differential scanning calorimeter and X-ray diffraction study were used to study crystalline and amorphous behavior. Analysis of design space showed that process was robust with the particle size less than 200 nm and EE up to 78%. Results of stability studies showed stability of carrier in various storage conditions and in different pH condition. From all the above study, it can be concluded that NLCs may be suitable carrier for the delivery of BCM with respect to stability and quality attributes.

<p>Formulation design, characterization, and in vitro and in vivo evaluation of nanostructured lipid carriers containing a bile salt for oral delivery of gypenosides</p>

“…DSC is a basic method to investigate the crystallization or amorphous state of drugs and NLCs by confirming the change of energy and temperature at phase transformation. 35 DSC thermogram data ( Figure 5) revealed that the cryoprotectant (mannitol) reached an endothermic peak with a high intensity of approximately 167.13°C, which was exactly the same melting point of mannitol. GPS and GMS reached endothermic peaks at 166.67°C and 57.15°C, respectively.…”

Development of pH-Dependent Nanospheres for Nebulisation- In vitro Diffusion, Aerodynamic and Cytotoxicity Studies

“…Optimized BDP loaded HPMC phthalate nanospheres were subjected to short term stability studies according to ICH Q1A (R2) guidelines [30][31][32]. It was performed at 40 ± 2 °C/ 75 ± 5 % RH in an environmental stability chamber over a period of 180 days to assess the stability of BDP loaded HPMC phthalate nanospheres.…”

Fabrication and characterization of shape memory polymers based bioabsorbable biomedical drug eluting stent

“…Low-magnification FESEM images are shown in Figure 4, it demonstrates the surface morphology of bare polymeric stent and drug-loaded polymeric stent. The surface topography of drug-eluting stents is considered as an important factor in stent performance (Kudarha et al 2015). Bare stents were associated with an increased intimal thickness, persistent intimal fibrin deposition, intraintimal hemorrhage and increased intimal adventitial inflammation (Lee et al 2007).…”

“…Hemolysis is the destruction of red blood cells. If hemolysis occurs in-vivo, it may causes anemia, jaundice and other pathological conditions (Kudarha et al 2015). Accordingly, to determine non-toxicity of stent in erythrocytes, hemolysis study was carried out.…”