Formulation and Evaluation of Chitosan-PLGA Biocomposite Scaffolds Incorporated with Quercetin Liposomes Made by QbD Approach for Improved Healing of Oral Lesions.

The current research aims to develop and evaluate chitosan-PLGA biocomposite scaffolds in combination with quercetin liposomes to accomplish the desired impact in oral lesions where pharmacotherapeutic agent treatment through circulation could only reach the low content at the target. Optimization of quercetin-loaded liposomes was carried out using 32 factorial design. The preparation of porous scaffolds comprising produced quercetin-loaded liposomes by thin-film method was carried out in the current study using a unique strategy combining solvent casting and gas foaming procedures. The prepared scaffolds were tested for physicochemical properties, in vitro quercetin release study, ex vivo drug permeation and retention research using goat mucosa, antibacterial activity, and cell migration studies on fibroblast L929 cell lines. Improved cell growth and migration were seen in the order control < liposomes < proposed system. The proposed system has been examined for its biological and physicochemical features, and it has the potential to be utilized as an efficient therapy for oral lesions.

In vitro targeting and selective killing of mcf-7 and colo320dm cells by 5-fluorouracil anchored to carboxylated SWCNTs and MWCNTs.

The intention of the present work was to synthesize the f-MWCNT and f-SWCNT terminated with proper functional group, loading of 5-Flurouracil and to perform cytotoxic activity. Functionalization of MWCNTs and SWCNTs was achieved through the acid treatment (H2SO4 + HNO3). 5-flurouracil was loaded into the prepared functionalized CNTs, thereafter; in vitro drug loading capacity and % drug release were calculated. Also the prepared f-CNTs, 5-flurouracil loaded CNTs were distinguished by using SEM, TGA, DSC, X-ray diffraction, Raman and FTIR spectroscopy. MCF-7 and COLO320DM cells were treated with selected concentrations of 5-FU loaded f-MWCNTs and f-SWCNTs to estimate the cytotoxic activity. It was observed that 5-FU loaded f-SWCNTs showed good activity against selected cell lines than others. Moreover, apoptosis percentage was reported to be 84.46 ± 4.3515 and 92.78 ± 2.6549 for 5-FU loaded f-SWCNTs against MCF-7 and COLO320DM cells respectively. It is evident from the results that the prepared drug loaded CNTs have comparable antitumor activity in cancer cell lines.

Green synthesis of silver, iron and gold nanoparticles of lycopene extracted from tomato: their characterization and cytotoxicity against COLO320DM, HT29 and Hella cell.

Our study aimed at development of Silver, Iron and Gold nanoparticles of Lycopene isolated from tomato by using green synthesis technique and to evaluate its anticancer potential against colorectal and cervical cancer. Lycopene was extracted by benzene extraction method and the silver, iron and gold nanoparticles were developed by green synthesis method. 1% aqueous extract of isolated Lycopene was mixed with 1% solutions of AgNO3, FeCl3 and HAuCl4 solutions and incubated at ambient temperature for 3-4 h separately and observed for the color change which is an indicative of formation of the nanoparticles. The prepared nanoparticles were characterized by FTIR, SEM, XRD analysis and evaluated for their antimicrobial potential. The cytotoxicity studies were carried out by in vitro assay like MTT, SRB and Tryphan blue method against Colo 320 DM, HT 29, and Hella. SEM showed nanosized particles of 50-100 nm range, whereas no antimicrobial activity was exhibited by the prepared nanoparticles. In MTT assay the LyAgNP showed maximum 41.41 ± 0.4124% inhibition against COLO320DM, whereas LyGNP exhibited 41.47 ± 0.4469% inhibition against HT 29 and LyAgNP showed 40.9 ± 0.6908% inhibition against Hella cells. In SRB assay LyAgNP showed maximum 82.68 ± 1.1798% inhibition against COLO320DM, whereas LyGNP exhibited maximum 91.21 ± 0.2372% inhibition against HT29 and 87.98 ± 0.5878% inhibition against Hella cells. In tryphan blue assay against COLO320DM, HT29 and Hella cells, the maximum inhibition exhibited by the prepared nanoparticles were observed as LyGNP 83.45 ± 0.4694%, LyAgNP 88.05 ± 0.1870% and LyAgNP65.47 ± 0.4766%. We conclude that the developed nanoparticles of Lycopene exhibited potential anticancer activity against Colorectal and cervical cancer cell as compared with pure Lycopene.

Colon targeted dosage form of Capecitabine using folic acid anchored modified carbon nanotube: in vitro cytotoxicity, apoptosis and in vivo roentgenographic study.

OBJECTIVE: Development of dosage form comprising of Capecitabine loaded carbon nanotubes for its targeted delivery to the colon. METHOD: Single walled carbon nanotubes (SWCNT) were functionalized by -COOH and Chitosan along with Folic acid. Capecitabine was loaded in these SWCNT's, and the system was analyzed by FTIR, SEM and Raman spectroscopy. Percent drug loading was assessed and the cytotoxicity (COLO320DM and HT29) was verified by using MTT and SRB assay. The apoptosis study was carried out by flowcytometry. The system was enclosed in an enteric coated capsule with pH sensitive polymers and characterized for invitro disintegration, dissolution and invivo roentgenographic studies. RESULTS: FTIR, Raman and XRD studies indicated the confirmation of attachments, whereas SEM exhibited size range of 200-500 nm. Drug loading capacity was observed to be 94.63 ± 1.07%. Cytotoxicity studies of Capecitabine and FA-CHI-F-SWCNT-Capecitabine against COLO320DM by using MTT assay showed that FA-CHI-F-SWCNT- Capecitabine exhibited 86.45 ± 0.5788% inhibition whereas pure Capecitabine showed 50.52 ± 0.3106% inhibition. Against HT29, the % inhibition was observed to be 82.76 ± 0.4668% and 56.41 ± 0.2316% respectively for FA-CHI-F-SWCNT-Capecitabine and pure Capecitabine. In case of SRB assay of COLO320DM, the FA-CHI-F-SWCNT-Capecitabine exhibited 89.62 ± 0.4095% inhibition and Capecitabine showed 84.36 ± 0.2559% inhibition, whereas against HT29, FA-CHI-F-SWCNT-Capecitabine showed 81.36 ± 0.2958% inhibition and Capecitabine exhibited 90.62 ± 0.4196% inhibition. CONCLUSION: FA-CHI-F-SWCNT loaded system revealed better cytotoxicity as compared with pure Capecitabine against two different cell lines. Invivo studies revealed that the prepared capsule formulation remained intact in the stomach thereby preventing drug release in the gastric milieu.

Optimization and validation of RP-HPLC method for simultaneous estimation of palbociclib and letrozole.

A simple, rapid, and robust RP-HPLC method have been developed and validated to measure palbociclib (PB) and letrozole (LT) at single wavelength (254 nm). A isocratic elution of samples performed on Intersil C8 (4.6 mm × 250 mm particle size 5 µm) column with mobile phase consisting 0.02 M sodium dihydrogen phosphate buffer (pH 5.5): acetonitrile: methanol (80:10:10 v/v/v) delivered at flow rate 1.0 mL min-1. A good linear response was achieved over the range of 5-50 µg mL-1. The LODs for PB and LT were found to be 0.098 and 0.0821 µg mL-1, while the LOQs for PB and LT were 0.381-0.315 µg mL-1, respectively. The method was quantitatively evaluated in terms of system suitability test, linearity, precision, accuracy (recovery) and robustness as per standard guidelines. The method is simple, convenient and suitable for the analysis of PB and LT in bulk drug.

Bioanalytical method development and validation for simultaneous estimation of cefixime and dicloxacillin by RP-HPLC in human plasma.

An accurate, rapid and simple reversed-phase high performance liquid chromatography (RP-HPLC) bioanalytical method was developed and validated for simultaneous estimation of cefixime, dicloxacillin in human plasma using ezetimibe as an internal standard. The cefixime, dicloxacillin and internal standard were extracted by liquid-liquid extraction technique. Chromatographic separation is accomplished using CAPCELL PAK C18 (4.6 mm × 250 mm, 5 m) analytical column. The mobile phase consisted of phosphate buffer, acetonitrile and methanol in 42:55:03 proportions. Detection and quantification were performed by UV/Vis detection at 225 nm. The lower limit of quantification was 0.5 µg mL(-1) for both cefixime and dicloxacillin in human plasma. The calibration curves were linear over the concentration range 0.5 to 40 µg mL(-1) for both drugs in human plasma. The method was quantitatively evaluated in terms of linearity, precision, accuracy, recovery, selectivity, and stability. The method was found to be simple, convenient and suitable for the analysis of cefixime and dicloxacillin from biological fluids.

Isolation and identification of hair growth potential fraction from active plant extract of Blumea eriantha DC grown in Western Ghat of India: In silico study.

BACKGROUND: In Aayurveda, Blumea eriantha DC has been used in the management of various diseases and is found to exhibit antioxidant and anti-hyperlipidemic, hypoglycemic, anti-diarrhoeal, larvicidal, antimicrobial properties. OBJECTIVE: The present study has focused on isolation of the active fraction from B. eriantha DC extract and to investigate its effect as a hair growth promoter along with identification of phytoconstituent(s) responsible for hair growth activity and its probable mechanism of action. MATERIALS AND METHODS: Our work introduces an effective isolation protocol for the active fraction from B. eriantha DC extract using chromatographic techniques. Fraction A was isolated by using mobile phase toluene:acetone (9:1). In-vitro and in-vivo methods were executed for the evaluation of hair growth activity. Moreover, the docked conformations of the isolated phytoconstituent Dimethyl sulfone was compared to Minoxidil for selected proteins namely 2FGF, 2PVC and 4U7P. The PDB identifications 2PVC (DNMT3L recognizes unmethylated histone H3 lysine 4), 4U7P (Crystal structure of DNMT3A-DNMT3L complex and 2FGF (Human Basic Fibroblast Growth Factor) were downloaded from Protein Data Bank. RESULTS: The study data revealed that B. eriantha DC alcoholic extracts exhibited prominent hair growth activity and it was affirmed that Dimethyl sulfone a phyto-constituent isolated from B. eriantha DC alcoholic extract contributed for the same. CONCLUSION: The findings strongly suggest hair growth promotion potential of the extract of B. eriantha DC.

In vivo and in vitro hair growth-promoting effect of silver and iron nanoparticles synthesized via Blumea eriantha DC plant extract.

BACKGROUND: Blumea eriantha DC is the Indian medicinal remedy, mainly distributed in the States of India. It possesses wide array of medicinal properties. AIM: To execute green synthesis approach for the preparation of silver and iron nanoparticles by using alcoholic Blumea ErianthaDC extract and to verify the biological potential of the prepared nanoparticles as a hair growth promoter. PATIENTS/METHOD: Extract was mixed with silver nitrate and ferric chloride for synthesis of silver and iron nanoparticles, respectively. Prepared nanoparticles were confirmed by UV, FT-IR, SEM, X-ray diffraction, and TEM. The qualitative and quantitative analysis was performed namely hair growth initiation, hair growth completion, hair length, hair weight, histopathological studies, skin thickness, and length of the hair follicle. RESULTS: The prepared nanoparticles were observed as a blend of spherical and irregular shape with an average particle size of 35nm. The transition of anagen hair follicles was observed in approximately 63.43 % of animals treated with Minoxidil, whereas 2% and 5% Blumea erianthasilver nanoparticles treated animal group exhibited 33.02% and 60.93%, respectively. The animal groups treated with 2% and 5% iron nanoparticles of Blumea Eriantha showed 44.09 and 38.89% in anagen induction, respectively, which suggest the hair growth-promoting potential of the extract of Blumea erianthaDC. CONCLUSION: Thus, it can be concluded that silver nanoparticles of Blumea Eriantha exhibit promising hair growth promoting activity.

Screening of hair growth promoting activity of Punica granatum L. (pomegranate) leaves extracts and its potential to exhibit antidandruff and anti-lice effect.

The intent of the present investigation was to explore the utility of alcoholic and aqueous extract of Punica granatum L. as hair growth promoter along with anti-lice and antidandruff activity. A filter paper diffusion approach was employed for screening of the pediculocidal and ovicidal activity. Albino mice, preselected for their telogen phase of hair growth were used during the study. The prepared extracts, Minoxidil and control were applied over shaved skin surface on to the backs of mice to assess telogen to anagen transition. The qualitative and quantitative analysis was performed. The outcome of the studies revealed that Punica granatum L. alcoholic and aqueous extracts exhibited prominent anti-lice activity. The transition of telogen to anagen phase of the number of anagen hair follicle was observed in approximately 45, 27 and 51% of animals treated with alcoholic and aqueous extract of Punica granatum L., and Minoxidil, respectively, which suggest the hair growth promoting potential of the extract of Punica granatum L. Also, 3 % Punica granatum L. alcoholic extracts exhibited a potent antidandruff activity against fungal strains tested. Maltol, was identified as a principal phytoconstituent in the alcoholic extract. The findings greatly suggest anti-lice, antidandruff and hair growth promoting potential of the extract of Punica granatum L.

Green synthesis of silver and iron nanoparticles of isolated proanthocyanidin: its characterization, antioxidant, antimicrobial, and cytotoxic activities against COLO320DM and HT29.

BACKGROUND: In the current research, we have developed silver and iron nanoparticles of isolated proanthocynidin (PAC) from grape seed by green synthesis and evaluated for antimicrobial, antioxidant activity and in vitro cytotoxicity against colon cancer cell lines. RESULTS: One percent solution of isolated proanthocynidin in water was vigorously mixed with 1% silver nitrate and 1% ferric chloride solution and kept for 4 h, to yield PACAgNP and PACFeNP. The synthesized nanoparticles were characterized by UV, FTIR, XRD, and SEM analysis and evaluated for antimicrobial potential against selected microbes. Moreover, the synthesized nanoparticles were studied for DPPH assay and in vitro cytotoxicity using colon cancer cell lines COLO320DM and HT29 (MTT, SRB, and Trypan blue assay). UV spectroscopy confirmed the development of nanoparticles. SEM analysis showed that the particles were aggregated in the size range of 50 to 100 nm. Antimicrobial potential was found to be less against Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli, whereas cytotoxicity of PACAgNP and PACFeNP against COLO320DM and HT29 exhibited promising results as compared to the pure PAC. PACAgNP and PACFeNP exhibited 20.83 ± 0.33% and 18.06 ± 0.60% inhibition, respectively, against DPPH radical, whereas pure PAC showed 16.79 ± 0.32% inhibition and standard (ascorbic acid) exhibited 98.73 ± 0.18% inhibition of DPPH radical. CONCLUSION: The silver and iron nanoparticles were successfully developed by green synthesis method using isolated proanthocynidin which is economical and eco-friendly. The use of metal nanoparticles may open up a new opportunity for anticancer therapies to minimize the toxic effects of available anticancer drugs specifically in targeting specific site.

Preparation of Arjunarista Using Microbes Isolated from Woodfordia fruticosa Flowers (Dhayati).

OBJECTIVE: To verify the utility of isolated fermentative microbes from Woodfordia fruticosa flowers for preparation of Arjunarista formulation and its comparative evaluation with the same formulation prepared by traditional method. METHODOLOGY: In the present technique, isolated colonies of microorganisms from Woodfordia fruticosa (Dhataki) flowers on Saubroad dextrose media were separated and suspended in sterile water. This suspension was aseptically added in previously sterilized mixtures containing all intended ingredients for Arjunarista which was thereafter incubated for 20 days at 37°C to achieve optimal fermentation. The formulation thus obtained was further subjected to various evaluation tests. RESULT: Arjunarista was prepared using a new approach, and in that, isolated microorganisms from the flowers of Woodfordia fruticosa (Dhataki) were used. It was found that the new approach was successful in generating approximately same quantities of alcohol content in comparison with traditional methods which have shown varying concentration of alcoholic content. Moreover, the new process prevents the growth of unwanted microbes thus, optimizing standards for purity and safety of the formulation. CONCLUSION: The formulation prepared by a new procedure showed marked uniformity for different parameters such as alcohol production, total phenol content, total solid content as compared to that prepared by the traditional method. Similarly, the results of thin layer chromatography, high performance thin layer chromatography showed marked uniformity related to quality, safety, efficacy, and reproducibility of the new method as compared to the traditional one. Thus, the modern technique was found to show reproducibility and facilitate easier quality assessment.

Screening of in-vitro hypoglycemic activity of Murraya koenigii and Catharanthus roseus / Cribado de la actividad hipoglucémica in vitro de Murraya koenigii y Catharanthus roseu

Objective: The study aimed to verify the hypoglycemic effect of Murraya koenigii (M. koenigii) and Catharanthus roseus (C. roseus) by using various in-vitro techniques. Method: The extracts were studied for their effects on glucose adsorption capacity, in-vitro glucose diffusion, in-vitro amylolysis kinetics and glucose transport across the yeast cells. Results: It was observed that the extracts of M. koenigii and C. roseus adsorbed glucose and the adsorption of glucose increased remarkably with an increase in glucose concentration. There were no significant (p≤0.05) differences between their adsorption capacities. In the amylolysis kinetic experimental model the rate of glucose diffusion was found to be increased with time from 30 to 180 min and both the plant extracts exhibited significant inhibitory effects on the movement of glucose into external solution across the dialysis membrane as compared to control. The extracts also promoted glucose uptake by the yeast cells and the enhancement of glucose uptake was dependent on both the sample and glucose concentration. The extract of M. koenigii exhibited significantly higher (p≤0.05) activity than the extract of C. roseus at all concentrations used in the study. Our report suggests the mechanism(s) for the hypoglycemic effect of M. koenigii and C. roseus. Conclusion: The said effect was observed to be mediated by inhibiting alpha amylase, inhibiting glucose diffusion by adsorbing glucose and by increasing glucose transport across the cell membranes as revealed by in-vitro model of yeast cells. However, these effects need to be affirmed by using different in vivo models and clinical trials

Objetivo: El estudio tuvo como objetivo verificar el efecto hipoglucémico de Murraya koenigii (M. koenigii) y Catharanthus roseus (C. roseus) mediante el uso de diversas técnicas in vitro. Método: Los extractos se estudiaron por sus efectos sobre la capacidad de adsorción de glucosa, la difusión de glucosa in vitro, la cinética de amilolisis in vitro y el transporte de glucosa a través de las células de levadura. Resultados: se observó que los extractos de M. koenigii y C. roseus adsorbieron glucosa y la adsorción de glucosa aumentó notablemente con un aumento en la concentración de glucosa. No hubo diferencias significativas (p≤0.05) entre sus capacidades de adsorción. En el modelo experimental cinético de amilolisis, se encontró que la velocidad de difusión de glucosa aumentaba con el tiempo de 30 a 180 min y ambos extractos de planta exhibían efectos inhibitorios significativos sobre el movimiento de la glucosa hacia la solución externa a través de la membrana de diálisis en comparación con el control. Los extractos también promovieron la absorción de glucosa por las células de levadura y la mejora de la captación de glucosa dependió tanto de la muestra como de la concentración de glucosa. El extracto de M. koenigii exhibió una actividad significativamente mayor (p≤0.05) que el extracto de C. roseus en todas las concentraciones utilizadas en el estudio. Nuestro informe sugiere el mecanismo (s) para el efecto hipoglucemiante de M. koenigii y C. roseus. Conclusión: Se observó que dicho efecto estaba mediado por la inhibición de la alfa amilasa, la inhibición de la difusión de glucosa por la adsorción de glucosa y el aumento del transporte de glucosa a través de las membranas celulares según lo revelado por el modelo in vitro de células de levadura. Sin embargo, estos efectos deben ser afirmados mediante el uso de diferentes modelos in vivo y ensayos clínicos

In vitro hypoglycemic effects of unripe and ripe fruits of Musa sapientum

ABSTRACT The present study was undertaken to verify the hypoglycemic potential of unripe and ripe fruit extracts of Musa sapientum by using various in-vitro techniques, namely glucose adsorption capacity, glucose diffusion, amylolysis kinetics and glucose transport across the yeast cells. The results revealed that the unripe and ripe fruit extracts of Musa sapientum adsorbed glucose and the adsorption of glucose increased remarkably with an increase in glucose concentration. There were no significant (p≤0.05) differences between their adsorption capacities. In the amylolysis kinetic experimental model the rate of glucose diffusion was found to be increased with time from 30 to 180 min and both extracts exhibited significant inhibitory effects on the movement of glucose into external solution across the dialysis membrane as compared to control. The plant extracts also promoted glucose uptake by the yeast cells and enhancement of glucose uptake was dependent on both the sample and glucose concentration. The hypoglycemic effect exhibited by the extracts was observed to be mediated by inhibiting α-amylase, inhibiting glucose diffusion by adsorbing glucose and by increasing glucose transport across the cell membranes as revealed by an in-vitro model of yeast cells.