Fabrication, appraisal, and transdermal permeation of sildenafil citrate-loaded nanostructured lipid carriers versus solid lipid nanoparticles

Abstract

Although sildenafil citrate (SC) is used extensively for erectile dysfunction, oral delivery of SC encounters many obstacles. Furthermore, the physicochemical characteristics of this amphoteric drug are challenging for delivery system formulation and transdermal permeation. This article concerns the assessment of the potential of nanomedicine for improving SC delivery and transdermal permeation. SC-loaded nanostructured lipid carriers (NLCs) and solid lipid nanoparticles (SLNs) were fabricated using a modified high-shear homogenization technique. Nanoparticle optimization steps included particle size analysis, entrapment efficiency (EE) determination, freeze-drying and reconstitution, differential scanning calorimetry, in vitro release, stability study and high-performance liquid chromatography analysis. Transdermal permeation of the nanocarriers compared with SC suspension across human skin was assessed using a modified Franz diffusion cell assembly. Results revealed that SLNs and NLCs could be optimized in the nanometric range (180 and 100 nm, respectively) with excellent EE (96.7% and 97.5%, respectively). Nanoparticles have significantly enhanced in vitro release and transdermal permeation of SC compared with its suspensions. Furthermore, transdermal permeation of SC exhibited higher initial release from both SLN and NLC formulations followed by controlled release, with promising implications for faster onset and longer drug duration. Nanomedicines prepared exhibited excellent physical stability for the study period. Solid nanoparticles optimized in this study successfully improved SC characteristics, paving the way for an efficient topical Viagra ® product.

Preparation, characterization, and in vivo pharmacokinetics of nanostructured lipid carriers loaded with oleanolic acid and gentiopicrin

“…20 The samples were then analyzed by HPLC. Control experiments were performed in the same way using the same proportions of gentiopicrin and oleanolic acid as in the GONLCs to investigate drug release behavior.…”

The Impact of Variables on Particle Size of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers; A Comparative Literature Review

“…Size stability results revealed that both SLNs and NLCs kept their particle size during 6 months of storage, demonstrating the good physical stability of the particles. 33 Souto et al prepared clotrimazole-loaded SLN with Dynasan® 116 as the solid lipid and NLC with the same lipid accompanied by 30% Miglyol® 812 as the oil. Their results showed no significant difference in size between NLC and SLN produced with the same total lipid and surfactant composition.…”

Novel piperine-loaded Tween-integrated monoolein cubosomes as brain-targeted oral nanomedicine in Alzheimer’s disease: pharmaceutical, biological, and toxicological studies

“…6,[14][15][16][17][18][19][20][21][22] Lipidbased liquid crystalline nanoparticles (LCN) have recently captured the obvious interest of pharmaceutical research to enhance the bioavailability of lipophilic drugs. 23 LCN enjoy characteristics of biocompatibility, bioadhesivity, and biodegradability offering various advantages for brain delivery.…”