Concentrations Of Piperine Research Articles

Regulatory Effects of Apatinib in Combination with Piperine on MDM-2 Gene Expression, Glutathione Peroxidase Activity and Nitric Oxide level as Mechanisms of Cytotoxicity in Colorectal Cancer Cells.

Purpose: Apatinib has been utilized in colon cancer therapies but its efficiency and molecularmechanism are not fully understood. Chemotherapy in combination with non-toxic compoundscan be an effective treatment strategy for cancer. Consequently, this study was carried out toevaluate the effects of apatinib and piperine on colorectal cancer (CRC) cell line and theirpotential anti-cancerous mechanisms in vitro. Methods: The effects of apatinib and piperine on HCT-116 CRC cells were detected byassessing cell viability using MTT assay. The potential cytotoxic mechanisms of apatinib andpiperine were investigated by evaluating MDM-2 gene expression ratio using real-time PCRassay. Moreover, the glutathione peroxidase (GPX) activity and nitric oxide (NO) levels wereassessed by colorimetric assays. Results: The proliferation rate of CRC cells decreased by increasing the concentrations ofpiperine or apatinib. When HCT-116 cells were treated with different concentrations of apatinibin combination with piperine, the synergistic effects were observed (combination index < 1).In HCT-116 cells treated with apatinib and piperine at the concentrations of 0.5×IC50 and0.2×IC50, the MDM-2 gene expression was downregulated and NO levels increased comparedto the untreated control cells and related single treatments. In addition, GPX activity significantlydecreased in combination treatment at 0.5×IC50 concentration of both agents versus singletreatments. Conclusion: Apatinib in combination with piperine could significantly inhibit the growth ofCRC cells. These cytotoxic effects were induced by regulation of MDM-2 gene expression andinhibition of antioxidant marker.

Determination and risk characterisation of bio-active piperine in black pepper and selected food containing black pepper consumed in Korea.

Piperine is a bio-active compound found in pepper, including Piper nigrum L. and P. longum L. It has a strong, pungent flavour and several pharmacologic benefits. However, the risks of piperine have not yet been characterized. In this study, piperine in black pepper and some selected foods was determined to characterise the risk of exposure to piperine. Piperine in black pepper, curry and noodle was analysed by high-performance liquid chromatography-ultraviolet detection, which was validated through the measurement of performance parameters. The mean concentrations of piperine in black pepper, powdered curry, retorted curry, instant noodle and cup noodle were 4,418, 28, 3.4, 4.3 and 4.2mg/100g, respectively. The estimated dietary exposure to piperine was 123.66μg/kg body weight/day, and the margin of exposure calculated by the no-observed-adverse-effect level of piperine, was 162. The piperine from food does not cause an adverse health effect to the public in Korea.

Cytogenotoxicity and protective effect of piperine and capsaicin on meristematic cells of Allium cepa L.

Piperine and capsaicin are important molecules with biological and pharmacological activities. This study aimed to evaluate the cytogenotoxic and protective effect of piperine and capsaicin on Allium cepa cells. A. cepa roots were exposed to negative (2% Dimethylsulfoxide) and positive (Methylmethanesulfonate, MMS, 10 µg/mL) controls, and four concentrations (25-200 µM) of piperine or capsaicin (alone) or associated before, simultaneously or after with the MMS. Only the lowest concentration of piperine (25 µM) showed a protective effect because it was not genotoxic. Piperine and capsaicin were cytotoxic (50, 100 and 200 µM). Piperine (50 to 200 µM) caused a significant increase in the total average of chromosomal alterations of in A. cepa cells. For capsaicin, the genotoxic effect was dose-dependent with a significant increase for all concentrations, highlighting the significant presence of micronuclei and nuclear buds for the two isolates. In general, bioactive compounds reduced the total average of chromosomal alterations against damage caused by MMS, mainly micronuclei and/or nuclear buds. Therefore, the two molecules were cytotoxic and genotoxic at the highest concentrations, and did not have cytoprotective action, and the lowest concentration of piperine demonstrated important chemopreventive activity.

A Validated Stability-indicating RP-HPLC Method for Piperine Estimation in Black Pepper, Marketed Formulation and Nanoparticles

Abstract: Aim: The aim of the study was to develop and validate a simple stability indicating reversephase High Performance Liquid Chromatography (RP-HPLC) method for quantitative analysis of piperine in Ayurvedic marketed formulation, black pepper and cubosome nanoformulation. Methods: The method was established by using Luna C18 HPLC column using a mobile phase consisting of acetonitrile: 0.01% ortho phosphoric acid (60:40, v/v; pH 3), delivered isocratically with flow rate of 1 mL/min and detected at 340 nm. The validation of chromatographic parameters and stress testing were performed in accordance with International Conference on Harmonization (ICH) guidelines. Results: The developed method was observed to be specific, linear (r2 > 0.999) over the selected range of concentration 0.5 to 20 μg/mL, precise (percentage relative standard deviation < 2%), with the detection and quantification limit as 0.015 and 0.044 μg/mL respectively. The relevancy of the developed method was analyzed on the piperine entrapped cubosome nanoformulation, which was formulated by fragmentation technique. The entrapment efficiency of piperine for prepared cubosome was observed to be 87.01 %. The method was implemented for the estimation of piperine in black pepper. The concentration of piperine in marketed formulation was found to be similar with the labeled concentration. The analyte peak was found to be complete resolved without any interference of additives and degrading products. Conclusion: The validated method was observed to be specific, sensitive and sufficient for the routine analysis of food products, marketed formulations and nanoparticles containing piperine.

Antioxidant and anti-inflammatory effects of piperine on UV-B-irradiated human HaCaT keratinocyte cells

The increase in intracellular reactive oxygen and nitrogen species plays a key role in ultraviolet B (UV-B)-induced inflammatory responses in the human skin. Piperine exhibits many pharmacological benefits. In the present study, the photoprotective effects and the possible underlying mechanisms of the anti-inflammatory effects of piperine on UV-B-irradiated keratinocytes were investigated. Piperine exerted strong, direct scavenging effects on DPPH radicals and exhibited free radical scavenging capabilities as demonstrated by the DCFH-DA and Griess assays. Consistent with these results, 10, 20, and 40 μM piperine pretreatments attenuated UV-B irradiation-induced keratinocyte cytotoxicity as reported by the resazurin assay. The highest concentration of piperine inhibited UV-B irradiation-induced cell apoptosis, as revealed by Hoechst 33342 staining. Moreover, we demonstrated the anti-inflammatory effects of piperine using western blot analysis, real-time PCR, and ELISA. Pretreatment with piperine suppressed the activation of phosphorylated p38, JNK, and AP-1 as well as the levels of COX-2/PGE2 and iNOS synthesis, while UV-B-irradiated cells triggered the induction of these signaling molecules. These results indicated that the inhibition of these inflammatory signaling pathways might play a key role in the regulation of the anti-inflammatory effects of piperine. In addition, piperine showed stronger anti-inflammatory effects than celecoxib which served as a positive control at the same concentration. All these results suggested that the anti-inflammatory properties of piperine protected keratinocytes from UV-B-induced damage, which might be due to its antioxidant properties. Therefore, piperine may be an effective therapeutic candidate compound for the treatment of UV irradiation-induced skin inflammation.

Inactivation of Salmonella on black peppercorns using an integrated ultraviolet-C and cold plasma intervention

A nonthermal process that applies ultraviolet (UV)–C and helium cold plasma (CP) simultaneously (UV-CP) has been investigated as an intervention technology to inactivate Salmonella on black peppercorns. The optimum CP treatment voltage and UV-CP treatment time for inactivating Salmonella on black peppercorns were predicted using a model equation as 9.7 kV and 22.1 min, respectively, which non-thermally inactivated Salmonella by 3.7 log CFU/g. UV-CP treatment yielded a stronger bactericidal activity than UV treatment alone, without inducing photoreactivation. In addition, UV-CP-induced reactive species were similar to those found in individual UV and CP treatments. Furthermore, UV-CP treatment caused a profound deformation of Salmonella morphology and a greater extent of DNA damage than UV or CP treatment did alone. UV-CP treatment did not alter the color or 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging activity; however, it lowered the 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity and piperine concentration in the peppercorns. The findings of this study demonstrate the potential application of UV-CP treatment for decontamination of black peppercorns.

Synthesis and Characterisation of Piperine-loaded Starch Nanoparticles

This study aimed to explore the potential application of starch nanoparticles as the nanocarriers for the controlled release of piperine. Starch nanoparticles with mean particle sizes ranging from 50 nm to 200 nm have been synthesised as nanocarriers for encapsulation of piperine. Piperine has been successfully loaded onto starch nanoparticles via the in-situ nanoprecipitation method. The loading capacity of piperine was affected by the synthesis conditions such as types and concentrations of surfactants as well as initial piperine concentrations. Under optimum conditions, starch nanoparticles exhibited a maximum piperine loading capacity of 4.74 mg mg–1. Piperine was observed to release out from starch nanoparticles in a slow and steady manner over a period of 168 h under physiological pH.

Delivery of Apoptosis-inducing Piperine to Triple-negative Breast Cancer Cells via Co-polymeric Nanoparticles.

Piperine, a major alkaloid of the fruit of black pepper plants, selectively inhibits the growth of triple-negative breast cancer cells but its lipophilicity restricts possible clinical application. This study therefore determined the feasibility of encapsulating piperine in nanoparticles (NPs) to increase its solubility in an aqueous environment. Piperine-loaded biodegradable methoxy poly(ethylene glycol)-poly(lactic-co-glycolic) acid copolymer-based NPs were produced by single emulsion solvent extraction and thin-film hydration. Growth and viability of triple-negative breast cancer (TNBC) cells were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and Annexin-V-FLUOS/propidium iodide staining, respectively. Thin-film hydration was superior to single emulsion solvent extraction, yielding piperine-loaded NPs with an average size of 50 nm. Piperine-loaded NPs inhibited TNBC cell growth and induced apoptosis while sparing normal fibroblasts. It is feasible to deliver a cytotoxic concentration of piperine to TNBC cells via NPs with the potential for improved bioavailability and solubility in biological fluids.

Pharmacokinetics of piperine after oral administration of Sahastara remedy capsules in healthy volunteers.

Background and purpose:To investigate the pharmacokinetics of piperine after single oral doses of capsules containing Sahastara (SHT) remedy dried ethanolic extracts in healthy Thai volunteers.Experimental approach:Twenty-four healthy volunteers were divided into two dosage groups. They received a single oral dose of SHT remedy extract capsules of 100 or 200 mg. Blood was collected at time intervals of 0, 0.5, 1, 2, 4, 6, 8, 12, 24, and 48 h. Acute clinical safety was monitored by complete physical examination and laboratory tests during the study period. Piperine concentration in blood and urine was determined by liquid chromatography tandem-mass spectrometry.Findings/Results:No serious adverse events were detected, only one volunteer had abdominal pain that was self-limiting. The pharmacokinetics of piperine following SHT remedy extract capsule administration demonstrated a mean peak concentration (Cmax) of piperine of 3.77 μg/mL and 6.59 μg/mL after dosing with 100 and 200 mg, respectively. Interestingly, a secondary maximum concentration of piperine was observed in this study, which might be related to enterohepatic recirculation. Negligible amounts of unchanged piperine were detected in urine.Conclusion and implication:The systemic exposure of piperine after SHT remedy ethanolic extract demonstrated dose proportionality after single oral dosing of 100-200 mg. Piperine was detectable in plasma for at least 48 h with evidence of enterohepatic recirculation. Metabolism and excretion profiles of piperine after administration of SHT remedy extract capsule need to be further explored for phytopharmaceutical product development.

Piperine synergistically enhances the effect of temozolomide against temozolomide-resistant human glioma cell lines

ABSTRACT Temozolomide (TMZ) is an alkylating chemotherapy agent used in the clinical treatment of glioblastoma multiforme (GBM) patients. Piperine (PIP) is a naturally occurring pungent nitrogenous substance present in the fruits of peppers. We investigated the anti-cancer efficacies of PIP alone and in combination with TMZ in GBM cellsusingparameters such as cell proliferation, cellular apoptosis,caspase-8/-9/-3 activities, cell cycle kinetics, wound-healing ability, and loss of mitochondrial membrane potential (MMP). Treatment with PIP and alow concentration of PIP-TMZ, inhibited cell growth, similar to TMZ.PIP-TMZ promoted apoptosis by activation of caspase-8/-9/-3, MMP loss, and inhibition of in vitro wound-healing motility. Reverse transcription polymerase chain reaction analysis showed significant inhibition of Cyclin-dependent kinases (CDK)4/6−cyclin D and CDK2−cyclin-E expression upon treatment with a low concentration PIP-TMZ, suggesting an S to G1 arrest. Our findings provide insight into the apoptotic potential of the combination of a low concentration of PIP-TMZ, though further in vivo study will be needed for its validation.

Bioautography and GC-MS based identification of piperine and trichostachine as the active quorum quenching compounds in black pepper

In the search of new and safe antibacterial compounds, the quorum sensing system (QS) modulation by natural products has been studied. As a result, many plant-derived compounds have been identified as potent quorum sensing inhibitors. Piper nigrum L. (black pepper) ethanolic extract inhibits the QS in some Gram-negative bacteria but the active components have not been previously identified. Thus, the objective of this work was to identify the P. nigrum peppercorns main components that block the QS, applying bioassay and chromatographic techniques. Piperine and trichostachine were identified as the main components responsible for the quorum quenching (QQ) activity of P. nigrum peppercorns extract. Piperine at 30 mg/L, decreased the violacein production by Chromobacterium violaceum CV026 by 35%, without affecting bacterial growth. Piperine concentration of 40 mg/L decreases violacein production by C. violaceum CV026 by 70% and growth in only 4.34%. Trichostachine at 50 mg/L decreases violacein production by C. violaceum CV026 by 12%, without affecting bacterial growth. P. nigrum extract concentration of 0.5 g/L decreased violacein production in 40 % and no effects on growth were observed. Neither P. nigrum extract, piperine, nor trichostachine did affect QS of Pseudomonas aeruginosa PAO1. Data here described exhibit the potential of piperamides as modulators of QS, not previously reported.

Metabolomics signatures of acutely ill and short-term weight recovered women with anorexia nervosa.

Although metabolomics studies are recently spreading and have allowed the characterization of putative biomarkers in many diseases, they are relatively scanty in anorexia nervosa (AN). In this explorative study we analyzed the fecal metabolomics profiles of women with AN in the underweight phase (n = 24) and after short-term weight restoration (n = 16) and compared them with 20 healthy women. An untargeted metabolomic procedure allowed the characterization of 224 metabolites involved in energy, lipid, and amino acid metabolism. A partial least square discriminant analysis identified 14 metabolites with a variable importance in projection score >1.5 that clearly differentiated underweight from weight-restored patients from healthy women. Compared with healthy women, fecal concentrations of valeric acid and 3-methyl,2-ketobutyric acid were increased in both underweight and weight-restored patients; fecal concentrations of propionic acid, stearic acid, linolenic acid, methyl-galactoside, coprosterol, cycloserine, and lauric acid were increased while fecal levels of xylose, fucose, and rhamnose were decreased in underweight patients and normalized after weight-restoration; fecal concentrations of piperine, phenylalanine, butyric acid, and meso-erythritol-1 were decreased while fecal levels of hydroxystearic acid were increased in weight-restored but normal in underweight AN patients. All these changes point to peculiar fecal metabolomics profiles of acute and short-term weight restored AN patients. The value of these changes to improve our understanding of the pathophysiology of AN and to characterize potential biomarker targets for developing new treatment strategies needs further studies to be clarified.

Piperine inhibits the transformation of endothelial cells into fibroblasts

Objective: To investigate the role of piperine on the transformation of endothelial cells into fibroblasts. Methods: Cultured human umbilical vein endothelial cells (HUVECs, 4-6 passage) were used for the main experiments. The transformation models of endothelial cells into fibroblasts were induced by transforming growth factor β (TGF-β) stimulation. HUVECs were divided into 6 groups: control group, TGF-β group and 4 groups treated with various concentrations of piperine (1, 5, 10, 20 μmol/L). CKK-8 was used to detect cell proliferation. The CD31/α-smooth muscle actin (α-SMA) expression level was detected by fluorescent staining. The vascular endothelial cadherin (VE-cadherin)/vimentin expression was detected by immunofluorescence staining. RT-PCR was used detect the mRNA expressions of transformation markers. Western blot was used to detect the protein expression of snail and twist. Results: TGF-β increased HUVECs proliferation (P<0.05), which could be significantly inhibited by 10 and 20 μmol/L of piperine, but not by 1 and 5 μmol/L of piperine. Immunofluorescence results demonstrated that TGF-β increased HUVECs transformation to fibroblasts as shown by downregulated expression of endothelial markers CD31, VE-cadherin, and upregulated expression of α-SMA and vimentin, again, these effects could be attenuated by 10 and 20 μmol/L piperine. The expression levels of collagen type Ⅰ and type Ⅲ were significantly higher in TGF-β group than in control group (P<0.05), significantly lower in TGF-β+10 μmol/L piperine group and TGF-β+20 μmol/L piperine group than in TGF-β group (P<0.05).In addition, RT-PCR results showed that TGF-β increased mRNA expression of transformation markers (snail1, snail2, twist1, twist2), while 10 and 20 μmol/L of piperine could significantly downregulated the mRNA expressions of these markers. The protein expression levels of snail and twist were significantly higher in TGF-β group than in control group (both P<0.05), which was significantly lower in TGF-β+20 μmol/L piperine group than in TGF-β group (both P<0.05). Conclusions: Piperine can inhibit the transformation of endothelial cells into fibroblasts. This effect might be viewed as one of the potential mechanisms of reduced myocardial fibrosis post piperine treatment.

Piperine blocks voltage gated K+ current and inhibits proliferation in androgen sensitive and insensitive human prostate cancer cell lines

Piperine is an attractive therapeutic alkaloid from black pepper that exhibits a broad spectrum of pharmacological properties over various pathological disorders including cancer. Voltage gated K+ (KV) channels play an important role in regulating cancer cell proliferation and are considered as potential target for cancer treatment. However, the implication of piperine in KV associated anticancer activities on human prostate cancer cells LNCaP and PC-3 remains unrevealed. The electrophysiological and pharmacological data identifies that both androgen sensitive (LNCaP) and insensitive (PC-3) prostate cancer cells typically expressed voltage gated K+ current (IK). This current was significantly blocked by piperine in a concentration-dependent manner with an IC50 value 39.91 μM in LNCaP and 49.45 μM in PC-3 cells. Analysis of voltage-dependence of activation kinetics showed that piperine induces a positive shift in the relative activation curve in both the cells. Piperine also depolarized the resting membrane potential by an average of 10.2 mV and 8.3 mV in LNCaP and PC-3 cells, respectively. The anticancer studies showed that, treatment with piperine concentration dependently induced G1 phase cell cycle arrest and apoptosis in LNCaP and PC-3 cells. These results unravel that the IK inhibition might be responsible for the anticancer effect of piperine on androgen sensitive and insensitive human prostate cancer cells.

Analysis of piperine content in cabe jawa extracts (Piper retrofractum Vahl) using UV spectrophotometry and HPLC

Cabe Jawa (Piper retrofractum Vahl) is an important commodity for herbal industries in Indonesia. One of the bioactive compounds in this herb is piperine. In this study, concentration of piperine in Cabe Jawa was analysed using HPLC and UV spectrophotometry methods. Cabe Jawa samples were prepared using two different methods. The first sample (S1) was dried from fresh Piper retrofractum, while the second sample (S2) was dried from boiled Piper retrofractum. Both samples were extracted using Soxhlet, followed by solvent evaporation to obtain the concentrated extract. Piperine concentration was measured using UV spectrophotometry and HPLC via internal standard method. The yields of extract of S1 and S2 were 23.0% and 22.1%, respectively. Piperine UV spectrophotometry standard curve equation was y = 0.1107*(X)-0.1578, R2 = 0.9999, whereas HPLC standard curve equation was y = 105916*(X) + 28100.9, R2 = 0.9978. Piperine concentration in S1 and S2 extracts quantified using UV spectrophotometry were 19.0% and 18.1%., respectively. The values for S were much higher compared to values obtained by HPLC, which were 6.8% (S1) and 7.3% (S2). Therefore, the use of UV spectrophotometry for analysis of piperine is not recommended due to the interference of other compounds, which are absorbed at the same wavelength.

Encapsulación de la piperine presente en la especie Piper tuberculatum utilizando vesículas multilamelares y determinación de su poder antioxidante

La piperina, alcaloide presente en la especie vegetal pipilongo (Piper tuberculatum) a la cual se le asocian propiedades antioxidantes, fue encapsulada en vesículas multilamelares (MLV). Para ello se realizó la validación de la metodología de extracción a través de curvas de calibración de piperina estándar por cromatografía líquida de alta resolución (HPLC) utilizando una columna C18, fase móvil MetOH:H2O (70:30) y detectada por UV a 340 nm con una tasa de flujo de 0.7 mL/min. El rango lineal y linealidad fueron halladas entre 1 a 300 ppm, con R2 de 0.995. En la extracción del fruto de pipilongo se estudió el efecto de dos factores, disolventes y potencia de ultrasonido, para la optimización de condiciones y mayor extracción de piperina en pipilongo. La máxima concentración de piperina (246.50 ppm) fue encontrada en las condiciones de ultrasonido (US 20 KHz a 175W, 40 min) utilizando etanol como disolvente de extracción. Del extracto, se aisló la piperina utilizando una solución de KOH 10% etanólico. Fue purificada y caracterizada mediante punto de fusión, IR, GC-MS y RMN 1H. Una vez obtenido el extracto, se procedió a la formación de liposomas. Las vesículas de fosfatidilcolina y colesterol fueron preparadas con extracto y con piperina a diferentes concentraciones e hidratadas con buffer PBS a pH 7.40. El tamaño promedio de las partículas formadas, medido por dispersión de luz dinámica (DLS), estuvo en un rango de 299.7–531.9 nm. Para el estudio de la actividad antioxidante, se preparó una solución de DPPH 0.2 mM y se llevó a reacción con los liposomas de extracto y de piperina y sus correspondientes formas libres durante 60 min, medidos a 520 nm. El IC50 calculado para el extracto y la piperina fueron 2.8±0.2 y 21333±1499 ppm, respectivamente. Estos valores de IC50 fueron comparados frente a un estándar de referencia preparado bajo las mismas condiciones, quercetina (IC50 2.5±0.1 ppm). El ensayo con DPPH mostró que la forma liberada posee mayor actividad antioxidante mientras que en la encapsulación atenúa y estabiliza esta capacidad.

UV-Vis Spectroscopy to Enable Determination of the Dissolution Behavior of Solid Dispersions Containing Curcumin and Piperine

Objective: Curcumin and piperine exibit poor aqueous solubility and dissolution. Solid dispersion technology is a promising way to improve dissolution of lipophilic compounds. Therefore, to investigate the dissolution behavior, an accurate determination of curcumin and piperine concentrations in a sample containing 0.5 wt-% SLS in sodium phosphate buffer as the dissolution medium was required. The goal of research was to investigate whether UV-Vis spectroscopy can be used to accurately determine curcumin and piperine concentrations in aqueous solutions. Method: Stock solutions (1 mg/mL) of curcumin and piperine were prepared in methanol. A series of solutions for calibration were prepared by mixing the stock solutions in various ratios after which they were diluted with dissolution medium (0.5%-wt sodium lauryl sulfate in 20 mM phosphate buffer; pH 6.0). Solutions of curcumin (2μg/mL) and piperine (1 μg/mL were subjected to overlay scan in a UV-VIS spectrophotometer in each λmax of 430 and 335.5 nm for curcumin and piperine, respectively. The method was validated according ICH requirements, such as specificity, linearity, accuracy, precision, limit of detection and limit of quantification. Results: At a concentration range of 0.1 to 5μg/mL, calibration curves of curcumin and piperine showed linearity with R2 = 0.9980 and 0.9982, respectively. Precision and accuracy was confirmed by AOAC. Furthermore, LOD of both compounds was 0.23 μg/mL and LOQ of curcumin and piperine was 0.72 and 0.69μg/mL, respectively. Conclusion: UV-Vis spectroscopy can be used to accurately determine curcumin and piperine concentrations in dissolution samples obtained during screening the dissolution behavior of solid dispersions containing these compounds. Key words: Curcumin, Piperine, Dissolution, UV-Vis spectroscopy.

Effect of piperine on size, shape and morphology of hydroxyapatite nanoparticles synthesized by the chemical precipitation method

The role of piperine, a water insoluble alkaloid compound on the nucleation, crystallinity, size, shape and dispersion of hydroxyapatite (HAp) nanoparticles was investigated. Two different concentrations of piperine were used as an organic modifier. FTIR spectra support the transformation of functional groups. The XRD pattern reveals the crystalline nature of the materials. The TEM images disclose the mechanism of nucleation, formation, shape, size and morphology of HAp nanorods. The addition of the piperine during the synthesis altered the morphology of HAp nanorods. Piperine, as water insoluble alkaloid could affect the morphology of the HAp nanoparticles with agglomeration. These types of well defined and shaped HAp nanorods can be used as a delivery service for drug release and in the field of biomaterial research.

UV SPECTROPHOTOMETRIC DETERMINATION OF PIPERINE IN NAVASAYA CHURNA: A POLYHERBAL FORMULATION

Navayasa Churna is an important ayurvedic formulation, is mentioned in Bhaishajyaratnavali in Pandu roga chikitsa iscombination of Nine i.e. Amlaki, Bibhitaka, Haritaki, Marica Pippali, Sunth, Chitraka, Musta, Vidanga and Lauha bhasma. The formulation is dispensed for the treatment of Anemia (pandu), Hepatoprotective and Liver disorders. The method for spectrophotometric determination of piperine from the fruits of Piper longum, Piper nigrum and Navasaya Churna has been developed at absorption maxima 342.7nm. The concentration of piperine present in raw material was found to be 2.981 ± 0.38 % (w/w) in marica and 0.981 ± 0.047 % (w/w) in pippali, respectively and in three identical laboratory batch of Navasaya churna name NY-I, NY-II, and NY-III, was 0.223 ± 0.34, 0.219 ± 0.42, 0.215 ± 0.43 % (w/w), respectively with mean value 0.219 ± 0.903 % (w/w). The piperine content of all the three batches is found to be in close proximities with each other.

Efficient brain uptake of piperine and its pharmacokinetics characterization after oral administration

1. Piperine, the major biological active component in black pepper has been associated with miscellaneous pharmacological effects, especially on central nervous system. To correlate with its neurological activity, a comprehensive pharmacokinetic profile of piperine in brain, plasma and cerebrospinal fluid after oral administration in rats was investigated in this study.2. It was noted that piperine could efficiently penetrate and homogeneously distribute into brain with similar pharmacokinetics profiles in each region. In addition, piperine concentrations in brain and plasma were found to be comparable with brain to plasma area under curve extrapolated to infinity (AUC0→∞) ratios of 0.95 and 1.10 for total concentration and unbound concentrations, respectively. Piperine also demonstrated high affinity toward brain tissue (98.4–98.5%) and plasma protein (96.2–97.8%) leading to a brain distribution volume of 36.32 ± 1.40 ml/g brain. Moreover, its efficient membrane permeability (Papp values of 5.41 ± 0.40 × 10- 5 cm/s and 4.78 ± 0.16 × 10- 5 cm/s for basolateral to apical and apical to basolateral transport in Caco-2 monolayer model) and limited hepatic metabolism (Clint of 8.15 μl/min/mg) could also contribute to its quick and high extent brain exposure.3. In summary, this study for the first time demonstrated high brain penetration potency of piperine could be resulted from its high brain tissue affinity and membrane permeability together with its limited liver metabolism.