Solid nanostructured lipid carriers loaded with silymarin for oral delivery: Formulation development and evaluation

Abstract

The present study was aimed at preparing stable dry adsorbed nanoparticles (DANs) of silymarin loaded nanostructured lipid carriers (NLCs). The prepared silymarin loaded NLCs and DANs were characterized for various quality parameters. Silymarin loaded NLCs were prepared by a modified hot melt emulsification ultra-sonication method using glyceryl monostearate (GMS), capmul MCM C8 EP (CAP) and gelucire 50/13 (G50/13) as solid lipid, liquid lipid and surfactant respectively. For better stability, NLC dispersion was converted into DANs by adsorbing them onto some suitable carriers. NLCs and DANs were characterized for particle size, polydispersity index, zeta potential, entrapment efficiency, drug loading, assay, thermal behavior, crystallinity and morphological study. The optimized NLCs have a mean particle size of 206.1±012.5 nm (size distribution of 0.249±0.058), a zeta potential of -32.5±1.2 mV with high entrapment of 95.60±0.45% and drug loading of 1.90±0.08%. The X-ray diffraction and endothermic peaks confirmed the maximum encapsulation of active in lipid matrices. The particles were spherical with smooth surface morphology. In-vitro release studies showed sustained drug release for up to 24 h. Ex-vivo permeation in the presence and absence of lymphatic blocker indicates the uptake of silymarin loaded NLCs by the lymphatic route. Silymarin loaded NLCs prepared had a nanosize distribution with high entrapment efficiency. The ex-vivo permeation study for optimized NLC formulation exhibited the lymphatic uptake of active. Dispersion stability was increased by preparing the DANs. The solid dry powder is used for oral reconstitution and can be further converted into tablets or filled into capsules.

Self-microemulsifying drug delivery system as carrier for the oral delivery of glimepiride: Formulation development, optimization, in-vitro characterization, stability assessment, ex-vivo permeation, and in-vivo antidiabetic activity in albino mice

“…It was also mentioned that lipid-based systems frequently experience lymphatic uptake, which enhances absorption and bioavailability even more. Because glimepiride belongs to the BCS class II group and hence has strong permeability, the permeation difference between suspension and SMEDDS was not particularly significant (10,24). These findings of antidiabetic activity align with previous research on solid nano dispersion (1) and micro emulsion (25) of glimepiride, which aimed to improve its bioavailability.…”

“…This carrier is characterized by its substantial surface area and effective adsorption capabilities. The method employed for this transformation was physical adsorption (10). The procedure involved combining the carrier with the emulsion in a 1:1 ratio within a glass mortar.…”

“…A non-everted gut sac model of chicken intestinal (jejunum) segments was utilized to conduct an ex-vivo intestinal permeability study (10,11). The segments underwent a thorough cleansing process with purified water to eliminate mucous and luminal contents.…”

Lipid-Based Nanoparticles in Delivering Bioactive Compounds for Improving Therapeutic Efficacy

“…Hirlekar and co-workers fabricated NLCs of silymarin by glyceryl monostearate, capmul MCM C8 EP, and gelucire 50/13 as the appropriate solid lipid, liquid lipid, and surfactant using improved hot melt emulsification and ultrasonication. However, the ex vivo permeability with and without a lymphatic inhibitor demonstrates lymphatic absorption of silymarin-loaded NLCs [ 114 ].…”