This article aimed to improve the relative solubility and dissolution rate of ferulic acid (FA) by the use of spray-dried solid dispersions (SDs) in order to ensure its in vitro antioxidant potential and to enhance its in vivo anti-platelet effect. These SDs were prepared by spray-drying at 10 and 20% of drug concentration using polyvinylpyrrolidone K30 (PVP-K30), polyethylene glycol 6000 (PEG 6000) and poloxamer-188 (PLX-188) as carriers. SDs and physical mixtures (PM) were characterized by SEM, XRPD, FTIR spectroscopy and TGA analysis. Spray-dried SDs containing FA were successfully obtained. Relative solubility of FA was improved with increasing carrier concentration. PVP-K30 and PEG 6000 formulations showed suitable drug content values close to 100%, whereas PLX-188 presented mean values between 70 and 90%. Agglomerates were observed depending on the carrier used. XRPD patterns and thermograms indicated that spray-drying led to drug amorphization and provided appropriate thermal stability, respectively. FTIR spectra demonstrated no remarkable interaction between carrier and drug for PEG 6000 and PLX-188 SDs. PVP-K30 formulations had changes in FTIR spectra, which denoted intermolecular O-H•••O = C bonds. Spray-dried SDs played an important role in enhancing dissolution rate of FA when compared to pure drug. The free radical-scavenging assay confirmed that the antioxidant activity of PEG 6000 10% SDs was kept. This formulation also provided a statistically increased in vivo anti-platelet effect compared to pure drug. In summary, these formulations enhanced relative solubility and dissolution rate of FA and chosen formulation demonstrated suitable in vitro antioxidant activity and improved in vivo anti-platelet effect.
Some plant species show medicinal potential in atherosclerosis and other coronary diseases. Curcumin (CUR) is a yellow-colored phenolic compound from rhizomes of Curcuma longa L. that is mainly used as anti-inflammatory, antioxidant, and anticancer. Piperine (PIP) is an alkaloid from the fruits and the seeds of Piper nigrum L. and Piper longum L. It has several pharmacological activities, including the antioxidant and the immunomodulatory properties. PIP also increases the nutrients absorption. This review aims at investigating the effect of the CUR and PIP co-administration on the lipid profile and the cardiovascular events based on animal and human studies. This study was performed in the main scientific search bases. Among the 4,992 references found, 2,004 papers were initially chosen for the partial reading and 15 of them filled all the selection criteria for the entire reading. The CUR and PIP co-administration generally demonstrated positive effects on lipid profile in animals and humans by reducing total cholesterol, triglycerides, and LP(a) and by increasing HDL-c. In spite of no long-term clinical trial was carried out for investigating the effect of CUR and PIP co-administration on cardiovascular events, the reduction of glucose, AST, and ALP, and the increase of CAT and SOD were recorded as secondary serum markers to avoid the cardiovascular risk. Therefore, the studies usually report that co-administration of CUR and PIP shows efficacy for reducing serum lipids. The effect on preventing cardiovascular events by reducing the cardiovascular risk is lacking of direct evidence.
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