Sponge spicules are needle-like structures and used for dermabrasive treatment of the skin. This research aimed to develop an effective delivery system by using sponge spicules for enhancing skin permeation of bioactive proteins and growth factors from deer antler velvet (DAV). DAV was extracted by sonication and bioactivity studies were evaluated. The size of microspicules (MSs) was reduced and mixed with DAV extract cream. In vitro skin permeation was analyzed by using bovine serum albumin-fluorescein isothiocyanate conjugate (BSA-FITC) as a model macromolecular compound. For in vivo study, DAV extract formulations were applied on the skin of healthy humans, and effects were evaluated. Results showed that DAV extract containing proteins and growth factors increased the proliferation and migration of skin fibroblast cells. This extract was homogeneously mixed with spicule cream. Without blending, MS was 11.89 µm wide and 176.77 µm long; blending time exhibited short and broken MSs (MBs) for short blending (30 s) and fine powder (MF) for long blending (10 min). MS cream showed the highest permeation of BSA-FITC through the skin (2.26-fold enhancement), but it resulted in skin irritation. Therefore, MB cream that increased the permeation of BSA-FITC by 1.94-fold was not significantly different from MS formulations chosen for in vivo study. Applying DAV-containing MB cream on the skin for 14 d decreased the melanin content and erythema value but increased elasticity and hydration. Therefore, the MB-containing cream can enhance the macromolecule delivery through the skin, improve the skin properties, and avoid skin irritation.
The aims of this study were to investigate the skin regeneration potential of bioactive placenta (deer placenta (DP), goat placenta (GP), and porcine placenta (PP)) and fabricate bioactive extract-loaded dissolving microneedles (DMNs) as a dermal delivery approach. The placentas were water-extracted, and the active compounds were evaluated. Bioactivity studies were performed in dermal fibroblasts and keratinocytes. DMNs were fabricated to deliver the potent bioactive placenta extract into the skin. All placental extracts expressed high amounts of protein, growth factors (EGF, FGF, IGF-1 and TGF-β1), and amino acids. These extracts were not toxic to the skin cells, while the proliferation of fibroblast cells significantly increased in a time-dependent manner. GP extract that exhibited the maximum proliferation, migration, and regeneration effect on fibroblast cells was loaded into DMN patch. The suitable physical properties of DMNs led to increased skin permeation and deposition of bioactive macromolecules. Moreover, GP extract-loaded DMNs showed minimal invasiveness to the skin and were safe for application to human skin. In conclusion, placental extracts act as potent bioactive compounds for skin cells, and the highest bioactive potential of GP-loaded DMNs might be a novel approach to regenerate the skin.
Pueraria mirifica (PM) extract is locally used to promote hair growth. However, the effective transdermal delivery system should be prepared to deliver the extract through the skin barrier. The objective of this study was to develop solid lipid nanoparticles (SLN) containing PM ethanolic extract for hair growth promotion. The cell viability and proliferation of human follicle dermal papilla cells (HFDPCs) treated with PM extract were evaluated by MTT assay. SLN formulations were developed as a transdermal delivery system of the PM extract, compared with liposomes. The physicochemical properties of these nanoparticles were determined. The in vitro skin permeation study was also evaluated by Franz type diffusion cells. For the result, PM extract was a good safety herbal extract, which no cytotoxicity at the concentrations from 1 to 1,000 μg/ml. The cell proliferation of PM extract treated HFDPCs significantly increased in a dose-dependent manner, indicating the possibility to promote hair growth at the concentrations from 10 to 100 μg/ml. For formulation development, 5% (w/v) PM extract-loaded SLN exhibited small particle size (93.83 ± 0.32 nm) with narrow size distribution and negatively charged. This formulation had the highest percent entrapment efficiency (42.64 ± 0.47%), followed by SLN containing 1% (w/v) PM extract (8.84 ± 0.24%) and undetectable in liposomes. For the skin permeation result, SLN containing 5% (w/v) of PM extract could penetrate through the skin more than solution form. Therefore, the small particle size and high PM extract entrapped in SLN exhibited higher PM extract penetrated through the skin barrier and hair follicles than PM ethanolic extract solution. PM extract-loaded SLN might be an effective formulation for hair growth disorders treatment.
Deer antler velvets (DAVs) contain many growth factors and protein. To extract growth factor from DAV, the suitable method and material properties have to investigate. The aim of this study was to improve the growth factor content in DAV extract for using as a skin rejuvenation compound. Different extraction methods (such as ethanol extract, probe sonication and precipitation method) and material preparations (such as fresh, dried by freeze drier and dried by hot air oven with and without gramma ray) were performed to evaluate the total protein and insulin-like growth factor-1 (IGF-1). The suitable condition was choose to determine the antioxidant activity and effect on the skin properties (such as in vitro skin permeation and in vivo human studies). For the results, fresh DAV extracted by probe sonication method provided the significantly highest total protein (586.31 + 48.17 mg/g) and IGF-1 (31.32 + 10.55 ng/g) contents. At the concentration of 2,000 μg/ml, this extract was completely dissolved in water and exhibited the antioxidant potential nearly 50% inhibition. For skin permeation at 24 h, the skin treated with DAV extract showed 3.83 + 2.04% of protein permeated through skin. The skin elasticity and hydration significantly increased after applying DAV extract for 28 days. In conclusion, the DAV extract by using fresh DAV and probe sonication method exhibited high IGF-1 and protein content as well as an antioxidant potential, leading to improve the skin properties. This extract might play an important role in the skin rejuvenation product.
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