An in vivo study of Hypericum perforatum in a niosomal topical drug delivery system

Abstract

The active compounds present in Hypericum perforatum L. (Hypericaceae) include hyperforin, hypericins and flavonoids, which are assumed to be responsible for the activity of the extract in the treatment of wounds and scars. The present study aimed to incorporate H. perforatum extract standardized to a known content of phloroglucinols, naphthodianthrones and polyphenolic compounds into an effective transdermal drug delivery system capable of entrapping both lipophilic and hydrophilic constituents in the form of niosomal gels for wound treatment. An 80% ethanol extract (HE) was prepared on a pilot scale using DIG-MAZ. An HPLC-DAD holistic profile was established for HE and was standardized to contain 3.4 ± 4 rutin, 1.1 ± 3 chlorogenic acid, 0.5 ± 2 quercitrin, 2.8 ± 2 hyperforin, and 0.51 ± 3% w/w total hypericins. Niosomes were prepared using the modified reverse phase evaporation technique (REV). The wound healing effect of the gel was tested on 16 adult mongrel dogs. A significant decrease in the inflammatory cell count (18.4 ± 5.3) was recorded in the niosomal gel 1.5% NaCMC-treated group at the 7th day post wounding. It induced a marked regression in the inflammatory phase and enhanced the early beginning of the proliferative phase of wound healing. After 21 days, it showed complete re-epithelization, formation of new matrix fibers and significant reduction in the wound size, compared to the control and the Panthenol® 2% cream treated groups. This is the first study of H. perforatum in a niosomal topical drug delivery system.

Vesicular Nanocarriers for Phytocompounds in Wound Care: Preparation and Characterization

“…Acemannan from Aloe vera is a polysaccharide able to increase fibroblast proliferation, the release of KGF-1 and VEGF, and the synthesis of type I collagen, being an important agent for tissue re-epithelization and angiogenesis [ 20 ]. Another well-known plant with wound healing properties is Hypericum perforatum [ 21 , 22 ], which enhances the migration of fibroblasts, collagen deposition, and by the action of hyperforin, PC, that is also antibacterial, increases the re-epithelization [ 21 , 22 ].…”

“…Most of the biologically active PCs, mainly the flavonoids, phenolics, and glycosidic aglycones, have limited bioavailability in the cellular media [ 50 ]. To solve this problem, the encapsulation in VNs seems to bring benefits, because in this way, the drug penetration into cell membranes is facilitated, increasing the permeability of active substances and topical therapeutic effectiveness [ 21 , 29 ]. The choice of the topical system has a decisive role concerning the penetration into the epidermis and maintenance of the therapeutic concentration in the skin tissue for a determined period [ 44 , 48 ].…”

“…Additionally, the VNs are considered promising delivery systems due to the ability of the phospholipidic structure to mimic the structural component of the mammalian cell membrane. Thus, the active compounds can passively penetrate the lipophilic membrane without causing cell damage [ 21 , 29 ].…”

Vesicular Systems Used for Wound Healing

“…Also, the wound healing activity of Hypericum perforatum-loaded niosomes was evaluated on adult mongrel dogs [58]. Hypericum perforatum has wound healing and antiinflammatory activities by enhancing the migration of fibroblasts and collagen deposition.…”

Quality by Design Approach for Development and Optimization of Nitrendipine Loaded Niosomal Gel for Accentuated Transdermal Delivery

“…The vesicular size and polydispersity index of nitrendipine loaded niosomes were determined by photon correlation spectroscopy, using Zetasizer (Malvern version 7.11 at 25 °C instrument U. K), which is based on the principle of dynamic light scattering (DLS) method [31,32]. PDI was used to determine the width of size distribution and the value of PDI less than 0.4 indicates the homogenous and a monodisperse population [33,34].…”