Hyaluronic Acid Micelles for Promoting the Skin Permeation and Deposition of Curcumin

Abstract

Background The poor skin permeation and deposition of topical therapeutic drugs is a major issue in topical drug delivery, improving this issue is conducive to improving the topical therapeutic effect of drugs. Methods In this study, octadecylamine modified hyaluronic acid (OHA) copolymer was synthesized by amide reaction technique to prepare curcumin (CUR)-loaded micelles (CUR-M) for topical transdermal administration. CUR-M was successfully prepared by dialysis, and the formulation was evaluated for particle size, zeta potential, surface morphology, entrapment effciency (EE%), drug loading (DL), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR) and the in vitro drug release. Additionally, in vitro skin permeation and retention, in vivo topical analgesic and anti-inflammatory activity, and skin irritation were assessed. Results The mean drug loading (DL), drug entrapment efficiency (EE), hydrodynamic diameter and zeta potential of CUR-M were 8.26%, 90.86%, 165.64 nm and −26.85 mV, respectively. CUR-M was characterized by X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR), it was found that there was an interaction between CUR and OHA, and CUR existed in CUR-M in an amorphous form. CUR-M exhibited sustained release in 48 h and good stability at 4 °C for 21days. CUR-M could significantly increase the skin penetration and retention of CUR and had better analgesic and anti-inflammatory activities in vivo when compared with CUR solution. Hematoxylin-eosin staining results revealed that the transdermal penetration mechanism of CUR-M might be related to the hydration of stratum corneum by HA. In addition, CUR-M showed no skin irritation to mouse skin. Conclusion CUR-M might be a promising and safe drug delivery system for the treatment of topical diseases.

Curcumin alleviates hypertrophic scarring by inhibiting fibroblast activation and regulating tissue inflammation

“…28 However, for wounds that have completely healed with scar formation, topical drugs on skin surface are difficult to penetrate and deposit into the tissues underneath due to the epithelial barrier. 29 In the present study, injection of curcumin into scar solid at the early stage of hyperplasia markedly alleviated the degrees of scar elevation and collagen deposition in the rabbit ear scars, accompanied with no local adverse reactions. Therefore, we speculate that early injection of curcumin is likely to improve the prognosis for patients with continuous hypertrophic scarring, and multiple injections may be safe.…”

“…By blocking phosphorylase kinase and the NF‐κB pathway, smearing curcumin gel on burn wound can reduce inflammation, accelerate healing and prevent residual scarring 28 . However, for wounds that have completely healed with scar formation, topical drugs on skin surface are difficult to penetrate and deposit into the tissues underneath due to the epithelial barrier 29 . In the present study, injection of curcumin into scar solid at the early stage of hyperplasia markedly alleviated the degrees of scar elevation and collagen deposition in the rabbit ear scars, accompanied with no local adverse reactions.…”

Microemulsion-Based Keratin–Chitosan Gel for Improvement of Skin Permeation/Retention and Activity of Curcumin

“…Fluorescent images of mouse skin treated with Cur solution, Cur ME and CME-KCS gel for 1 and 6 h are shown in Figure 6. At 1 h, there was almost no Cur signal observed in the skin treated with the Cur solution, which might be due to the poor permeability of the Cur molecule [6], while the skin treated with Cur-ME and CME-KCS gel showed significant green fluorescence signals of Cur in the epidermis and dermis. The fluorescence intensity of the skin treated with Cur solution, Cur-ME and CME-KCS gel significantly increased with the extension of penetration time.…”

“…[5]. The main limitation of the topical application of Cur is its poor physical and chemical properties, such as poor water solubility (13.76 µg/mL) and skin permeability, which make it difficult to achieve effective therapeutic concentration through conventional dosage forms (such as solutions, ointments or creams) [6]. Various techniques or methods have been proposed to enhance the topical delivery of lipophilic drugs of Cur [7].…”

Dipeptide-1 modified nanostructured lipid carrier-based hydrogel with enhanced skin retention and topical efficacy of curcumin

“…Then the skin samples were respectively cut into pieces with scissor and immersed in 2 mL methanol for 24 h at 4 °C, subsequently placed in an ultrasound bath (KQ-250DE, Kunshan, China) for 3 h. Then it was refrigerated centrifuged at 10 000 rpm for 10 min and the supernatant was ltered by a syringe with a Millipore lter (0.22 mm). 7,25 The ltrate was analysed using the same HPLC method described above, and the cumulative amount of CUR retained in the skin per unit area was calculated.…”