Comparative study of nisoldipine-loaded nanostructured lipid carriers and solid lipid nanoparticles for oral delivery: preparation, characterization, permeation and pharmacokinetic evaluation

Abstract

Nisoldipine (ND) has low oral bioavailability (5%) due to first-pass metabolism. Previously, solid lipid nanoparticles (SLNs) of ND were reported. In this study, nanostructured lipid carriers (NLCs) of ND are developed to enhance the oral bioavailability. ND-NLCs were prepared using hot homogenization-ultrasonication method, using oleic acid and trimyristate as liquid lipid and solid lipid, respectively. Prepared NLCs are evaluated for an optimal system using measuring size, zeta potential, entrapment efficiency, in-vitro release and in-situ absorption studies. Further, in vivo pharmacokinetic (PK) studies of NLC were conducted in rats comparison with SLN and suspension as controls. Size, ZP and EE of optimized NLCs were found to be 110.4 ± 2.95 nm, -29.4 ± 2.05 mV and 97.07 ± 2.27%, respectively. Drug loaded into NLCs was converted to amorphous form revealed by differential scanning calorimeter (DSC) and X-ray diffractometry (XRD) technique and nearly spherical in shape by scanning electron microscopy (SEM) studies. Drug release and absorption of ND were prolonged from ND-NLCs and ND-SLNs. From the PK results, NLCs showed 2.46 and 1.09-folds improvement in oral bioavailability of ND compared with suspension and SLNs formulations, respectively. Taken together, the NLCs and SLNs are used as carriers for the enhancement of oral bioavailability of the ND.

Neuroprotective Effect of Ropinirole Lipid Nanoparticles Enriched Hydrogel for Parkinson’s Disease: In Vitro, Ex Vivo, Pharmacokinetic and Pharmacodynamic Evaluation

“…RP-SLN composed of 2.0% w/v of Dynasan-114 as solid lipid and RP-NLC composed of 1.25% w/v of Dyanasn-114 and 0.75% w/v of Caproyl 90 as liquid lipid, respectively. In general, solid lipid to liquid lipid ratio 3:1 is ideal for the preparation of NLC formulation [31].…”

“…RP-SLN and RP-NLC formulation was yielded by hot melt emulsification coupled with ultra-wave sonication method [31,32]. The composition of the optimized RP-SLN and RP-NLC formulation is presented in Table 1.…”

Ciprofloxacin Loaded Nanostructured Lipid Carriers Incorporated into In-Situ Gels to Improve Management of Bacterial Endophthalmitis

“…Higher EE in the NLCs is obtained due to the blending of solid and liquid lipids, creating a disordered structure that provides higher space for drug loading. Moreover, the drug is more soluble in liquid lipids than solid lipids [41,55].…”

Improving the Oral Bioavailability of an Anti-Glioma Prodrug CAT3 Using Novel Solid Lipid Nanoparticles Containing Oleic Acid-CAT3 Conjugates

“…These nanoparticles can be prepared without the use of organic solvents and can be easily scaled up from laboratory to large-scale manufacture [17]. Moreover, as a lipid-based drug delivery system, SLN has been known to control drug release [18], promote oral absorption of drugs, modify the pharmacokinetics and pharmacodynamics [19,20], enhance tissue or cell-specific targeting [21], adjust tissue distribution [20], and reduce side effects [22][23][24]. Hence, SLN could be a superior drug delivery system to load CAT3 and improve bioavailability.…”