Distribution of Liposome-Encapsulated Ingredients in Human Skin Ex Vivo

A biocompatible topical thermo-reversible hydrogel containing Pranoprofen (PF)-loaded nanostructured lipid carriers (NLCs) was studied as an innovative strategy for the topical treatment of skin inflammatory diseases. The PF-NLCs-F127 hydrogel was characterized physiochemically and short-time stability tests were carried out over 60 days. In vitro release and ex vivo human skin permeation studies were carried out in Franz diffusion cells. In addition, a cytotoxicity assay was studied using the HaCat cell line and in vivo tolerance study was performed in humans by evaluating the biomechanical properties. The anti-inflammatory effect of the PF-NLCs-F127 was evaluated in adult male Sprague Daw-ley® rats using a model of inflammation induced by the topical application of xylol for 1 h. The developed PF-NLCs-F127 exhibited a heterogeneous structure with spherical PF-NLCs in the hydrogel. Furthermore, a thermo-reversible behaviour was determined with a gelling temperature of 32.5 °C, being close to human cutaneous temperature and thus favouring the retention of PF. Furthermore, in the ex vivo study, the amount of PF retained and detected in human skin was high and no systemic effects were observed. The hydrogel was found to be non-cytotoxic, showing cell viability of around 95%. The PF-NLCs-F127 is shown to be well tolerated and no signs of irritancy or alterations of the skin’s biophysical properties were detected. The topical application of PF-NLCs-F127 hydrogel was shown to be efficient in an inflammatory animal model, preventing the loss of stratum corneum and reducing the presence of leukocyte infiltration. The results from this study confirm that the developed hydrogel is a suitable drug delivery carrier for the transdermal delivery of PF, improving its dermal retention, opening the possibility of using it as a promising candidate and safer alternative to topical treatment for local skin inflammation and indicating that it could be useful in the clinical environment.

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ID3024 Polymeric nanoparticles display bactericidal effect and selective fermentation for the treatment of acne vulgaris

Biomedical Research and Therapy ◽

10.15419/bmrat.v4is.244 ◽

2017 ◽

Vol 4 (S) ◽

pp. 34

Author(s):

Ming-Fa Hsieh

Keyword(s):

Human Skin ◽

Ex Vivo ◽

Polymeric Nanoparticles ◽

Acne Vulgaris ◽

Short Chain Fatty Acids ◽

Bactericidal Effect ◽

Skin Microbiome ◽

Poly Ethylene Glycol ◽

Effective Doses ◽

Poly Ethylene

The use of antibiotics in the treatment of acne in specific group (pregnant women) of patients can lead to serious complications. We have previously demonstrated that the nanoparticles made of block copolymers of poly (ethylene glycol) and poly(e-caprolactone) can inhibit the growth of Propionibacterium acnes (P. acnes), a bacterium highly associated with the progress of acne vulgaris in the human skin [Polymers 2016; 8, 321]. To reduce the amount of antibiotics used in the treatment of skin acne, we have further demonstrated that a bacterium in the human skin microbiome can utilize PEG-based polymers to produce various short-chain fatty acids (SCFAs) which suppressed the growth of P. acnes. PEG-based polymers were chosen as selective fermentation initiators which specifically induced the fermentation of the skin commensal bacterium but not P. acnes. Interestingly, PEG-based polymers can efficiently suppress the growth of P. acnes. An acne ex vivo explant was established by using acne biopsies collected from patients with acne vulgaris at the early and middle stages. The levels of pro-inflammatory interleukin (IL)-8 cytokine in early- and middle-staged acnes were significantly higher than those in healthy skins. Incubation of acne ex vivo explants with sucrose remarkably reduced the level of IL-8 and the number of P. acnes. Results from mouse studies revealed that PEG-based polymer functions as antibiotic adjuvants which can considerably reduce the effective doses of clindamycin, a clinically-used acne antibiotic

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