Potential Lipolytic Effect of Panduratin A Loaded Microspicule Serum as a Transdermal Delivery Approach for Subcutaneous Fat Reduction.

Boesenbergia rotunda (L.) Mansf contained a potent anti-obesity agent. The objectives of this study were to investigate the anti-adipogenesis and lipolysis effects of panduratin A from B. rotunda extract and develop extract-loaded lipolytic body microspicule (MS) serum. Panduratin A that was separated from the ethanolic extract of B. rotunda in fraction 3 (BP-3) were studied the bioactivity of 3T3-L1 preadipocyte cells. The extract-loaded MS serum was formulated and evaluated for safety and efficacy. The BP-3 extract containing panduratin A at 0.29 g per g of the extract was not toxic to the cells at concentrations lower than 10 µg/mL, and the antiadipogenesis and lipolysis effects of the BP-3 extract were strong at 10 µg/mL. To deliver bioactive panduratin A into and through the skin, MS serum was successfully formulated. Application of BP-3 extract-loaded MS serum to the human thigh for 14 d reduced the thigh circumference and increased skin hydration and firmness. Although the skin erythema was increased, no severe redness or pain was found. In conclusion, BP-3 extract acts as a potent bioactive compound to inhibit adipocyte cells, and the antiadipogenesis and lipolysis effects of BP-3 extract in MS serum might play an important role as a potential lipolytic body product for reducing human subcutaneous fat mass.

Development of Sponge Microspicule Cream as a Transdermal Delivery System for Protein and Growth Factors from Deer Antler Velvet Extract.

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.

A Novel Approach for Skin Regeneration by a Potent Bioactive Placental-Loaded Microneedle Patch: Comparative Study of Deer, Goat, and Porcine Placentas.

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-ß1), 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.

In Vitro Biological Activity and In Vivo Human Study of Porcine-Placenta-Extract-Loaded Nanovesicle Formulations for Skin and Hair Rejuvenation.

Porcine placenta extract (PPE) contains many water-soluble macromolecular compounds, such as proteins and growth factors, which have limited transportation through the skin. This study aimed to assess the effect of porcine-placenta-extract (PPE)-loaded nano-transdermal systems for skin repair and hair growth promotion. The potentials of the nanoformulation for cytotoxicity, cell proliferation, intracellular reactive oxygen species (ROS) reduction, lipoxygenase inhibition, intracellular inflammatory cytokine reduction, and cell aggregation were evaluated. PPE-entrapped niosome nanovesicles were produced by thin-film hydration and probe-sonication methods, followed by incorporation in a skin serum formulation. The physicochemical properties of the formulation were examined, and the efficacy of the serum formulation was elucidated in humans. The results showed that PPE had no toxicity and was able to induce cell growth and cell aggregation. In addition, PPE significantly decreased intracellular ROS, inhibited lipoxygenase activity, and reduced the production of intracellular tumor necrosis factor-α. In the in vivo human study, the PPE nanovesicles-loaded serum could improve skin properties by increasing skin hydration. Moreover, it was capable of promoting hair growth by increasing hair elongation and melanin index after application for one month. Consequently, the PPE nanovesicles-loaded serum was effective for skin anti-aging and hair rejuvenation.

Hair growth promoting effect of bioactive extract from deer antler velvet-loaded niosomes and microspicules serum.

Deer antler velvet (DAV) extract is important in stimulating the growth of skin and hair cells. The aim of this study was to develop DAV extract-loaded niosomes (NIs) and microspicules (MS) serum for effective hair growth. Bioactivities of DAV extract on human dermal papilla cells were studied. To develop protein delivery, NIs were prepared to entrap DAV extract and then loaded into MS serum (NI serum MS). Physicochemical properties and in vitro skin permeations were evaluated. The formulations were applied on human scalp and relative efficacies were evaluated. DAV extract at 2,000 µg/ml significantly enhanced cell proliferation and aggregation. DAV extract-loaded NI exhibited nanovesicle, narrow size distribution and negative surface charge. The vesicles were able to load into MS serum and showed significantly highest macromolecular protein permeation through the skin, with deposition into the deepest skin layer compared with other formulations. Applying the serum on human scalp for 14 and 30 days significantly enhanced hair elongation and melanin content, with increased skin hydration and decreased the erythema index, thereby promoting hair growth without skin irritation. NI serum MS containing DAV extract played an important role to deliver biomacromolecular protein through the skin and hair follicles, leading to effective hair growth.