<p>Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema</p>

Abstract

Background: Nanostructured lipid carriers (NLCs) are emerging as attractive drug carriers in transdermal drug delivery. The surface modification of NLCs with cell-penetrating peptides (CPPs) can enhance the skin permeation of drugs. Purpose: The objective of the current study was to evaluate the ability of the cell-penetrating peptide (CPP) polyarginine to translocate NLCs loaded with lornoxicam (LN) into the skin layers and to evaluate its anti-inflammatory effect. Methods: The NLCs were prepared using an emulsion evaporation and low temperature solidification technique using glyceryl monostearates, triglycerides, DOGS-NTA-Ni lipids and surfactants, and then six histidine-tagged polyarginine containing 11 arginine (R11) peptides was modified on the surface of NLCs. Results: The developed NLCs formulated with LN and R11 (LN-NLC-R11) were incorporated into 2% HPMC gels. NLCs were prepared with a particle size of (121.81±3.61)–(145.72±4.78) nm, and the zeta potential decreased from (−30.30±2.07) to (−14.66±0.74) mV after the modification of R11 peptides. The encapsulation efficiency and drug loading were (74.61±1.13) % and (7.92±0.33) %, respectively, regardless of the surface modification. Cellular uptake assays using HaCaT cells suggested that the NLC modified with R11 (0.02%, w/w) significantly enhanced the cell internalization of nanoparticles relative to unmodified NLCs ( P <0.05 or P <0.01). An in vitro skin permeation study showed better permeation-enhancing ability of R11 (0.02%, w/w) than that of other content (0.01% or 0.04%). In carrageenan-induced rat paw edema models, LN-NLC-R11 gels inhibited rat paw edema and the production of inflammatory cytokines compared with LN-NLC gels and LN gels ( P <0.01). Conclusion: In our investigation, it was strongly demonstrated that the surface modification of NLC with R11 enhanced the translocation of LN across the skin, thereby alleviating inflammation.

<p>Berberine-Loaded Nanostructured Lipid Carriers Enhance the Treatment of Ulcerative Colitis</p>

“…47 Studies have shown that nanoscale drugs were taken up to a greater extent than free drugs. 48,49 In our uptake study, BBR-NLCs showed superior uptake compared with free BBR (Figures 1 and 5). In addition, qualitative analysis of uptake in vitro showed that BBR was distributed in the cytoplasm and nucleus, which was consistent with the findings of a study by Serafim.…”

Formulation and characterization of lornoxicam-loaded cellulosic-microsponge gel for possible applications in arthritis

“…Topical application of drug loaded gel (containing Transcutol P as permeation enhancer) with and without microneedles followed the concentration pattern, with higher drug concentration, higher was the efficacy. Furthermore, the results also clearly indicated that the use of microneedle significantly improved the effectiveness of drug loaded gel at the dose of 0.05 mL from 43% to 51% (p < 0.01) and at the dose of 0.1 mL from 65% to 72% ( Wang et al, 2017 , Gao et al, 2019 ). This enhancement was attributed to the disturbance of stratum corneum with microneedles, which allowed drug molecules to rapidly permeate the skin and resulted in quick therapeutic effect ( Al-Mayahy et al, 2019 ).…”

Cell-Penetrating Peptides in Diagnosis and Treatment of Human Diseases: From Preclinical Research to Clinical Application

“…Gao et al prepared lornoxicam-loaded lipid gels by R11 modified (LN-NLC-R11) to treat rat paw edema. LN-NLC-R11 significantly improved cellular uptake of NLC in HaCaT cells, remitted rat paw edema, and inhibited the inflammatory cytokines production than NLC in vivo (Gao et al, 2019). Due to steric hindrance, the distance between CPPs and nanoparticles will influence the efficiency of cellular internalization.…”