Application of film-forming solution as a transdermal delivery system of piperine-rich herbal mixture extract for anti-inflammation.

Piperine-rich herbal mixture (PHM) used in this study is a traditional Thai medicine that contains 21 oriental herbs. It is called "Sahastara remedy" and is officially included in the Thai National List of Essential Medicine since A.D. 2011. PHM has been used orally to relieve muscle and bone pains. It contains Piper nigrum fruits as a major constituent and also Piper retrofractum fruits, PHM thus has anti-inflammatory activities that mostly come from the bioactivities of piperine consisting of these pepper fruits. Unfortunately, PHM usually causes gastrointestinal side effects. Consequently, a topical product containing an alcoholic extract of PHM (PHM-E), i.e., film-forming solution (FFS) was developed to overcome this drawback. The aims of this study were to investigate the anti-inflammatory activity of PHM-E, to evaluate physicochemical properties and the anti-inflammatory activity of FFS containing PHM-E (PHM-E FFS). Anti-inflammatory activities of PHM-E were investigated in the RAW 264.7 cells. Physicochemical properties, in vitro toxicities and anti-inflammatory activities of PHM-E FFS including its dry film (PHM-E film) were determined. PHM-E showed anti-inflammatory activities with dose dependent manners via inhibition of nitric oxide and prostaglandin E2 production by the RAW 264.7 cells and promotion of the cell phenotype polarization from M1 to M2. PHM-E FFS had low viscosity and exhibited the Newtonian behavior. It provided elastic PHM-E film with low tensile strength. The release profile of piperine from PHM-E film followed a zero-kinetic model. PHM-E FFS demonstrated compatibility with the skin cells, minimal ocular irritant when accidentally splashing into the eye and moderate-to-high potency for inhibition of inflammatory symptoms in the rats. PHM-E FFS thus had potential for use in the further clinical study to investigate its efficacy and safety in patients.

Physicochemical properties of alpha-mangostin loaded nanomeulsions prepared by ultrasonication technique.

HYPOTHESIS: Alpha-mangostin (AMG) is a natural compound possessing strong antibacterial activity. Because of its poor water solubility, the formulations of AMG usually require high concentrations of solubilizers leading limitation for using in some clinical applications. Thus, the novel formulation of topical nanoemulsion (NE) containing AMG (AMG-NE) with optimal content of the oil phase and surfactants was developed. EXPERIMENTS: AMG was extracted, purified and used as an active ingredient of AMG-NE. Blank NEs (NEs without AMG) with varying in contents of the oil phase and surfactants and AMG-NE were prepared by the ultrasonication technique. They were investigated their physicochemical properties including antibacterial activity against Staphyloccocus aureus and Propionibacterium acnes (which is recently renamed as Cutibacterium acnes). FINDINGS: Blank NEs and AMG-NE had droplet size in a range of nanometer and negative value of zeta potential. The droplet size, polydispersity index and zeta potential of blank NEs were affected by formulation compositions and sonication intensities. AMG could be loaded into a representative Blank NE at a maximum concentration of 0.2% w/w and did not cause significant changes in physicochemical properties. AMG-NE showed the antibacterial activity against Staphyloccocus aureus and Propionibacterium acnes without toxicity to the skin cells. Therefore, AMG-NE had potential for using in a clinical study to investigate its efficacy and safety in patients.