Fabrication Of Solid Lipid Nanoparticles Research Articles

Rheumatoid Arthritis Treatment Potential of Stearic Acid Nanoparticles of Quercetin in Rats.

This study aims to assess the anti-inflammatory potential of stearic acid nanoparticles of quercetin in an arthritic rat model. This article describes the fabrication of solid lipid nanoparticles (SLNs) using the hot melt encapsulation method, followed by the anti-inflammatory study of SLNs and other characterizations such as FTIR, XRD, and SEM. Thirty male healthy albino rats were taken and treated with FCA to induce rheumatoid arthritis. Quercetin loading of quercetin to stearic acid was confirmed by FTIR. The efficacy of quercetin-loaded SLNs to reduce inflammation was evaluated with the help of inflammatory biomarker levels. Quercetin-loaded stearic acid nanoparticles were successfully prepared by using a hot melt encapsulation method. Their average size and zeta potential were 100 nm and -25 mV, respectively. Rheumatoid arthritis was significantly (p < 0.001) reduced in the quercetin-loaded SLN group, as indicated by finding out the reduced levels of inflammatory mediators such as tumor necrosis factor (TNF-α) and rheumatoid factor. Quercetin-loaded stearic acid nanoparticles were found to be potentially effective in treating RA.

Fabrication of solid lipid nanoparticles by hot high shear homogenization and optimization by Box–Behnken design: An accelerated stability assessment

Fabrication of solid lipid nanoparticles by hot high shear homogenization and optimization by Box–Behnken design: An accelerated stability assessment

Fabrication of solid lipid nanoparticles containing vitexin protects dopaminergic neurons against 6-hydroxydopamine induced Parkinson's disease model via altered the genetic backgrounds

Vitexin is a flavonoid which obtained from Crataegus pinnatifida Bunge. Further, its neuroprotective effects are examined in PD model. The motive of the current study was to fabricate vitexin loaded solid lipid nanoparticles and evaluate the effect against 6- hidroxidopamine (6-OHDA) induced parkinson's disease animal model. Intracerebroventricular injection of 6-OHDA was used for induction the PD and mice were treated with the said drug loaded nanocarrier for 28 days. In our study, hot melt emulsification and ultrasonication method was employed for the preparation of Vitexin loaded nanolipoidal carrier. Further, the enzymatic activities incudes Catalase (CAT), superoxide dismutase (SOD), glutathione (GSH) glutathione peroxidase (GPx), glutathione S-transferase (GST), level of reactive oxygen species, total reactive antioxidant dopamine and its metabolite homovanilic and 3, 4-dihydroxyphenylacetic acid, were determined in the striatum. Furthermore, the behavioural parameters including locomotor, memory and depressive were estimated. The Vitexin loaded solid lipid nanoparticles therapeutics in 6-OHDA induced Parkinson's, results clearly showed improvement in total reactive antioxidant, CAT, GPx, Dopamine and its metabolite level in striatum of mice. We also observed that reactive oxygen species in the striatum were diminished by solid lipid nanoparticles of Vitexin. Furthermore, the said formulation is well efficient in averting the memory destruction in Morris water maze test as well as depressive like behaviour in tail suspension test. Vitexin loaded solid lipid nanoparticles founds protective effects in neurodegeneration on 6-OHDA induced neurotoxicity in mice. In features, this could be alternative effective therapeutic approach for the management of PD.

Fabrication of solid lipid nanoparticles of lurasidone HCl for oral delivery: optimization, in vitro characterization, cell line studies and in vivo efficacy in schizophrenia

Objective: The aim of the present investigation was to investigate the efficacy of solid lipid nanoparticles (SLNs) to enhance the absorption and bioavailability of lurasidone hydrochloride (LH) following oral administration.Methods: The LH loaded SLNs (LH-SLNs) were prepared by high pressure homogenization (HPH) method, optimized using box Behnken design and evaluated for particle size (PS), entrapment efficiency (EE), morphology, FTIR, DSC, XRD, in vitro release, ex vivo permeation, transport studies across Caco-2 cell line and in vivo pharmacokinetic and pharmacodynamic studies.Results: The LH-SLNs had PS of 139.8 ± 5.5 nm, EE of 79.10 ± 2.50% and zeta potential of −30.8 ± 3.5 mV. TEM images showed that LH-SLNs had a uniform size distribution and spherical shape. The in vitro release from LH-SLNs followed the Higuchi model. The ex vivo permeability study demonstrated enhanced drug permeation from LH-SLNs (>90%) through rat intestine as compared to LH-suspension. The SLNs were found to be taken up by energy dependent, endocytic mechanism which was mediated by clathrin/caveolae-mediated endocytosis across Caco-2 cell line. The pharmacokinetic results showed that oral bioavailability of LH was improved over 5.16-fold after incorporation into SLNs as compared to LH-suspension. The pharmacodynamic study proved the antipsychotic potential of LH-SLNs in the treatment of schizophrenia.Conclusion: It was concluded that oral administration of LH-SLNs in rats improved the bioavailability of LH via lymphatic uptake along with improved therapeutic effect in MK-801 induced schizophrenia model in rats.

Enhanced intestinal absorption of asenapine maleate by fabricating solid lipid nanoparticles using TPGS: elucidation of transport mechanism, permeability across Caco-2 cell line and in vivo pharmacokinetic studies

The aim of the present investigation was to fabricate and evaluate solid lipid nanoparticles (SLNs) of asenapine maleate (AM) to improve its oral bioavailability (BA). AM-SLNs were prepared by high speed homogenization followed by ultrasonication technique. The resultant SLNs exhibited particle size, zeta potential and entrapment efficiency of 114.3 ± 3.5 nm, −12.9 ± 3.8 mV, and 84.10% ± 2.90% respectively. In vitro release study of AM-SLNs showed 9.23% ± 2.72% and 92.09% ± 3.40% release of AM in pH 1.2 medium and phosphate buffer pH 6.8, respectively, indicating higher potential of lymphatic uptake. Cell viability study using Caco-2 cell line indicated non-toxicity of the carriers and drug. The uptake of AM-SLNs across Caco-2 cell line was time and energy dependent exhibiting clathrin-claveole mediated endocytosis transport. Cellular uptake of Coumarin loaded SLNs was effectively increased as compared to the dye solution. The pharmacokinetic results in rats showed 50.19-fold improvement in BA of AM after fabrication of SLNs. Collectively, all these findings demonstrated effectiveness of SLNs to improve therapeutic efficacy of AM in the treatment of schizophrenia.

Development of efavirenz loaded solid lipid nanoparticles: Risk assessment, quality-by-design (QbD) based optimisation and physicochemical characterisation

The purpose of this study was development and characterisation of efavirenz (EFZ) loaded solid lipid nanoparticles (SLN) using QbD approach. Quality target product profile of EFZ loaded SLN were defined and critical quality attributes were identified. SLN were prepared by nanoprecipitation method. Initially, feasibility of SLN formation was studied by using different lipids including glyceryl monostearate, stearic acid and surfactants such as poloxamer 188, tween 80, docusate sodium and sodium lauryl sulphate. A 32 factorial design was employed to optimize EFZ loaded SLN wherein acetone/methanol ratio in organic phase and surfactant concentration were selected as independent variables whereas particle size (PS) and %entrapment efficiency (EE) were selected as responses. PS of SLN was found to be varied from 167.77 to 1166 nm and %EE was in the range of 23.07–88%. DSC thermograms indicated the amorphous state of EFZ in the SLN. The FTIR studies confirmed no interaction among materials used in fabrication of SLN while NMR studies confirmed their incorporation in the SLN. Spherical shape of SLN was confirmed by TEM. This study suggests the importance of implementation of QbD approach for identifying critical process and formulation parameter in order to develop nano based pharmaceutical product.