Formulation and optimization of solid lipid nanoparticles of buspirone HCl for enhancement of its oral bioavailability

Abstract

Solid lipid nanoparticles (SLNs) of buspirone HCl as a water-soluble drug were prepared by emulsification-evaporation, followed by the sonification method. A preliminary screening of the most effective parameters on the production of nanoparticles by a Taguchi L(8) orthogonal array showed that the lipid type, surfactant percentage, speed of homogenizer, and acetone:dichloromethane (DCM) ratio had a significant effect on particle size. In the next step, the lipid was fixed on cetyl alcohol, surfactant on Tween 20, lecithin:lipid weight ratio on 20:70, sonication time on 30 seconds, and the other effective, independent factors aforementioned were studied each at three levels by a three-factor, three-level Box-Behnken design. The percentage of drug entrapment, mean particle-size diameter, and zeta potential were studied as the responses. Contour plots were constructed to further elucidate the relationship between the independent and dependent variables. A pharmacokinetic study was conducted in male Wistar rats after oral administration of 15 mg.kg(-1) buspirone in the form of free drug or SLNs. The optimized SLNs had aq particle size of 345.7 nm, loading efficiency of 32.8%, and zeta potential of -6.8 mV. Buspirone released about 90% during 4.5 hours in vitro. It was found that the relative bioavailability of the drug in SLNs was significantly increased, compared to that of the drug solution.

Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

“…However, compared with BA-CMC, apparent V z , and CL z of BA were reduced in the case of BA-LP, which might result in a decrease in the chance of liver metabolism, to improve the oral bioavailability of BA. 41 In addition, the increased oral bioavailability of BA in the form of BA-LP might be attributed to the combination of several effects. [42][43][44] First, the particle size of BA-LP played a key role in the nanoparticle absorption rate -in general, the decreased particle size may improve the …”

Novel surface modified solid lipid nanoparticles as intranasal carriers for ropinirole hydrochloride: application of factorial design approach

“…300 ml of supernatant was then diluted to 3.0 ml with methanol and amount of free ROPI HCl in supernatant was determined spectrophotometrically at 250 nm using UVspectrophotometer (1700, Shimadzu Õ , Tokyo, Japan). DL and EE were calculated by using following Equations (2) and (3), respectively (Varshosaz et al, 2010):…”

Brain delivery of valproic acid via intranasal administration of nanostructured lipid carriers: in vivo pharmacodynamic studies using rat electroshock model

“…15,16 Briefly, the hot lipid phase at 60°C, containing 400 mg of CP, 100 mg of soy lecithin S100, 0.1 mL of octyldodecanol, and 400 mg of VPA, was dissolved in 10 mL of a mixture of three parts acetone and one part absolute ethanol in a water bath. The oily phase was then dispersed in 50 mL aqueous phase containing 1% Poloxamer 188 at 50°C and stirred for 1 minute at 2000 rpm.…”

“…Optimization of the nanoparticle formulations was carried out using Taguchi screening design and Box-Behnken analysis as reported earlier by the authors. 15,16 characterization of NLcs of VPA Photon correlation spectroscopy (Zetasizer 3000; Malvern Instruments, Malvern UK) was used to measure size and zeta potential of all drug-loaded NLC samples. All samples were diluted (1:10) with deionized water to get optimum 50-200 kilo counts per second for measurements.…”