Application of quality by design approach for intranasal delivery of rivastigmine loaded solid lipid nanoparticles: Effect on formulation and characterization parameters.
作者： Brijesh Shah , Dignesh Khunt , Himanshu Bhatt , Manju Misra , Harish Padh
DOI: 10.1016/J.EJPS.2015.07.002
关键词: Factorial experiment 、 Stereochemistry 、 Solid lipid nanoparticle 、 Chromatography 、 Quality by Design 、 Nasal administration 、 Particle size 、 Sonication 、 Chemistry 、 Pulmonary surfactant 、 High-performance liquid chromatography
摘要: In the present investigation, Quality by Design (QbD) approach was applied on development and optimization of solid lipid nanoparticle (SLN) formulation hydrophilic drug rivastigmine (RHT). RHT SLN were formulated homogenization ultrasonication method using Compritol 888 ATO, tween-80 poloxamer-188 as lipid, surfactant stabilizer respectively. The effect independent variables (X1 - drug: ratio, X2 concentration X3 time) quality attributes i.e. dependent (Y1 size, Y2 PDI Y3 %entrapment efficiency (%EE)) investigated 3(3) factorial design. Multiple linear regression analysis ANOVA employed to indentify estimate main effect, 2FI, quadratic cubic effect. Optimized formula derived from an overlay plot which further probe sonication evaluated. Final showed narrow size distribution (PDI- 0.132±0.016) with particle 82.5±4.07 nm %EE 66.84±2.49. DSC XRD study incorporation into imperfect crystal lattice ATO. comparison solution, higher in-vitro ex-vivo diffusion. diffusion followed Higuchi model indicating matrix due erosion. Histopathology intact nasal mucosa safety for intranasal administration.
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