Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Abstract

Aim: Breviscapine isolated from the Chinese herb Erigeron breviscapus (Vant) Hand-Mazz is widely used to treat cardiovascular and cerebrovascular diseases. The aim of this study was to improve the pharmacokinetic profiles of breviscapine using nanostructured lipid carrier based on an ionic complex formation. Methods: Breviscapine nanostructured lipid carrier (Bre-NLC) was prepared using the thin film homogenization method. The morphology of Bre-NLCs was determined using transmission electron microscopy. The mean particle size, polydispersity index, zeta-potential analysis and entrapment efficiency were analized. In vitro release was studied using the dialysis method. In vitro stability was studied in fresh plasma and liver slurry of rats. In vivo pharmacokinetics was analyzed in rats after intravenous injection of a dose equivalent to breviscapine (10 mg/kg). Results: The Bre-NLCs were spherical with a mean particle size of ~170 nm, a zeta potential of ~20 mV and a high entrapment efficiency of ~89%. Compared with a commercially available solution, a substantial decrease in the cumulative release of breviscapine was found for the Bre-NLCs. The NLC has a significantly protective effect against the liver enzyme degradation of breviscapine. After intravenous administration in rats, the Bre-NLCs exhibited a 32 times increase in the AUC 0-t and a 12 times increase in T 1/2 as compared to the commercially available breviscapine solution. Conclusion:The results demonstrate that the NLC has great potential to use as a novel sustained release system for breviscapine.

Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

“…This confirms that the release rate followed this order: SP suspension > SP LeciPlex F1 > SP LeciPlex F1 gel, which is consistent with the results shown in Figure 4. Previous studies showed that drug release from nanostructured lipid carriers had high correlation coefficient values for the Hixson-Crowell cube root equation [54]. In contrast, drug release data from SP gel, SP liposomes, and SP liposome gel were best interpreted by the Baker-Lonsdale model (Table 3).…”

Enhancing biopharmaceutical attributes of phospholipid complex-loaded nanostructured lipidic carriers of mangiferin: Systematic development, characterization and evaluation

“…Table 2 enlists the design matrix indicating thirteen experimental runs obtained for the NLCs, along with the factor levels in coded units and actual form. Prepared complex of Mgf was incorporated into the nanolipidic carriers through bottom-up approach, where the lipophilic complex was solubilized in the lipidic vehicle, used for the preparation of nanocarriers (Li et al, 2013;Beg et al, 2016). …”

Preparation and Characterisation of Nobiletin-Loaded Nanostructured Lipid Carriers

“…NOB-NLC was prepared through melt-emulsification technique and high-pressure homogenisation [21]. Briefly, 3 mL ethanol was added as cosolvent to the lipid phase, which was evenly composed of NOB, solid lipid, liquid lipid, and lecithin.…”

“…The EE of NOB-NLC was determined by measuring free NOB in the aqueous phase, which was separated using ultrafiltration centrifugation [21,25]. A total of 500 L NOB-NLC was added to the upper chamber of Centrifugal Filter Unit 100 kDa (Millipore Co., Boston, USA) and then centrifuged at 3000 rpm for 20 min at 4 ∘ C through UniCen MR (Herolab, Germany) [26].…”