Chitosan-telmisartan polymeric cocrystals for improving oral absorption: In vitro and in vivo evaluation.

This study describes the development of polymeric cocrystals of chitosan-telmisartan (TEL) to improve the oral bioavailability of TEL, which has poor oral solubility and bioavailability. The polymeric cocrystal was prepared using chitosan a biopolymer with the aid of sodium citrate as a salting-out agent. The cocrystals were characterized by FT-IR spectroscopy, scanning electron microscopy, differential scanning calorimeteri (DSC), thermogravimetric analysis (TGA), and powder X-ray diffraction (PXRD). The improved solubility of TEL was observed with cocrystals as compared to that of pure drug in solubility studies with phosphate buffer (pH 7.4). The in vivo pharmacokinetics properties of cocrystal were studied by an animal model using rats after a single dose oral administration. The results showed an increased plasma drug concentration (Cmax) of 1.47, µg/ml for cocrystals when compared to pure TEL with 0.96 µg/ml with one-fold increased bioavailability (F%) that is, the cocrystals increases the solubility of the drug and the paracellular drug absorption by tight junction modulation. Further the elimination constant Kel resulted with higher value of about 0.0085 h-1 when compared to pure drug with0.0048 h-1 along with improved AUC (14.62 µg/ml).

Capecitabine encapsulated chitosan succinate-sodium alginate macromolecular complex beads for colon cancer targeted delivery: in vitro evaluation.

The present study aims to investigate the efficacy of the novel biopolymeric complex multiparticulate system consisting of chitosan succinate and alginate for the capecitabine-targeted delivery to colon cancer. A Box-Behnken design was used to optimize the CS-SA beads by considering the effect of three factors: CS (A;X1), CaCl2 (B;X2), and SA (C;X3), on the response variables Y1 (EE), Y2 (Size), and Y3 (Release). The results of response surface plots allowed an optimized bead to be identified with high drug EE and maximum drug release at colon. The swelling index showed that the beads reached a maximum good swelling at pH 7.4, and nil or little swelling at acidic pH, which proves that the beads completely protect the release of drug. The in vitro release portrayed a maximum release at pH 7.4, due to the large swelling force that was created by electrostatic repulsion between the ionized carboxylic acid groups of the CS-SA network. In vitro cytotoxicity assay (MTT) of CS-SA beads shows inhibition of the proliferation of HT-29 tumour cell to induce apoptosis over a longer period of time. The above results show that CS-SA beads prolong the release of CP in the colonic region, and also enhance antitumor efficacy.

Extraction and identification of bioactive components in Sida cordata (Burm.f.) using gas chromatography-mass spectrometry.

Sida cordata (Burm.f.) is a pineal tropical plant in the family Malvaceae that is found throughout India and used to treat various diseases and ailments in many complementary and alternative medicine systems. This study identified the bioactive components present in whole-plant ethanol extracts of S. cordata using gas chromatography-mass spectrometry (GC-MS). Based on their retention times (RT) and mass-to-charge ratios (m/z), 29 bioactive compounds were identified: nonanoic acid, vitamin D3, 3-trifluroacetoxypentadecane, α-d-glucopyranoside, O-α-d-glucopyranosyl-(1.fwdarw.3)-α-d-fructofuranosyl,3,7,11,15-tetramethyl-2-hexadecan-1-ol, octadecanoic acid, ethyl ester, phytol, 9,12-octadecadienoic acid, methyl ester (E,E), 9,12,15-octadecadienoic acid, methyl ester (Z,Z,Z), oleic acid, 1,2-15,16-diepoxyhexadecane, 3-hexadecyloxycarbonyl-5-(2-hydroxyethyl)-4-methylimidazolium ion, methoxyacetic acid, 4-tetradecyl ester, 1,2-benzenedicarboxylic acid, mono (2-ethylhexyl) ester, 1-iodo-2-methylundecane, dodecane, 2,6,10-trimethyl-, 2-piperidinone-N-[4-bromo-n-butyl]-, squalene, octadecane-1-(ethenyloxy)-, Z,Z-2,5-pentadecadien-1-ol, 1-hexadecanol, 2-methyl-, spiro[androst-5ene-17,1'-cyclobutan]-2'-one-3-hydroxy-, (3a,17a)-, diethylene glycol monododecyl ether, vitamin E, cholestan-3-ol, 2-methylene-, (3a,5a)-, 2H-pyran, 2-(7-heptadecynyloxy)tetrahydro-, and cis-Z-α-bisabolene epoxide. The presence of various bioactive compounds justifies the use of this plant for treating various ailments by traditional practitioners.

Preparation, characterization, and in vitro diffusion study of nonwoven electrospun nanofiber of curcumin-loaded cellulose acetate phthalate polymer.

Novel curcumin (CUR)-loaded cellulose acetate phthalate (CAP) nonwoven electrospun nanofiber (NF) transdermal mat was developed and evaluated for its in vitro CUR diffusion properties. Various CAP solutions from 5 to 20 wt% were tested; 17.5 wt% was found to be a suitable concentration for NF fabrication without defects, such as bubble or ribbon structures. The selected wt% CAP solution was loaded with CUR and electrospun into NFs. The prepared CUR-loaded NFs were characterized using scanning electron microscopy, X-ray diffraction, ultraviolet-visible spectroscopy, thermogravimetric analysis (TGA), and in vitro diffusion studies. The as-prepared fibers demonstrated controlled in vitro transdermal delivery of CUR for up to 24 h.

Low-cost and eco-friendly green synthesis of silver nanoparticles using Prunus japonica (Rosaceae) leaf extract and their antibacterial, antioxidant properties.

Low cost and eco-friendly green synthesis of silver nanoparticles (AgNPs) from silver nitrate (AgNO3) using Prunus japonica leaves extract as reducing agent by a simple method at room temperature. The biosynthesized nanoparticles (NPs) were characterized by UV-Vis, tunneling electron microscopy (HR-TEM), scanning electron microscopy (SEM) coupled with X-ray energy dispersive spectrophotometer (EDAX), X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR). In UV-Vis spectroscopy results, the λmax was observed at 441 nm. The AgNPs synthesized were spherical, hexagonal, and irregular in shapes. The EDAX and XRD spectrum confirmed the presence of silver ions and crystalline nature of synthesized AgNPs. FTIR showed the functional groups such as C = O, N-H and C-N groups involved in the reduction of Ag+ to Ag. 2, 2-Diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay was performed and it showed the percentage inhibition in concentration-dependent manner. The synthesized AgNPs showed antibacterial activity against Escherichia coli, Proteus vulgaris, Staphylococcus aureus and Bacillus cereus to different extents and the higher activity was observed in Proteus vulgaris.

Chitosan cocrystals embedded alginate beads for enhancing the solubility and bioavailability of aceclofenac.

Enhanced oral bioavailability of aceclofenac has been achieved using chitosan cocrystals of aceclofenac and its entrapment into alginate matrix a super saturated drug delivery system (SDDS). Prepared SDDS were evaluated by various physiochemical and pharmacological methods. The result revealed that the primary cocrystals enhanced the solubility of the drug and the thick gelled polymer matrix that formed from swelling of calcium alginate beads makes it to release the drug in continuous and sustained manner by supersaturated drug diffusion. The Cmax, Tmax and relative bioavailability for aceclofenac cocrystal and aceclofenac SDDS were 2.06±0.42 µg/ml, 1 h, 159.72±10.84 and 2.01 µg/ml, 1 h, 352.76±12.91, respectively. Anti-inflammatory activity of aceclofenac was significantly improved with the SDDS. With respect to the results, it revealed that the SDDS described herein might be a promising tool for the oral sustained release of aceclofenac and likely for that of various other poorly soluble drugs.

Development of duloxetine hydrochloride loaded mesoporous silica nanoparticles: characterizations and in vitro evaluation.

This study investigated the potential use of mesoporous silica nanoparticles (MSNs) as a carrier for duloxetine hydrochloride (DX), which is prone to acid degradation. Sol-gel and solvothermal methods were used to synthesize the MSNs, which, after calcination and drug loading, were then characterized using X-ray diffraction (XRD), Brunauer-Emmett-Teller (BET) technique, thermogravimetric analysis (TGA), Fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and diffuse reflectance ultraviolet-visible (DRS-UV-Vis) spectroscopy. Releases of DX from the MSNs were good in pH 7.4 (90%) phosphate buffer but poor in acidic pH (40%). In a comparative release study between the MSNs in phosphate buffer, TW60-3DX showed sustained release for 140 h, which was higher than the other nanoparticles. The mechanism of DX release from the MSNs was studied using Peppas kinetics model. The "n" value of all three MSNs ranged from 0.45 to 1 with a correlation coefficient (r (2)) >0.9, which indicated that the release of the drug from the system follows the anomalous transport or non-Fickian diffusion. The results supported the efficacy of mesoporous silica nanoparticles synthesized here as a promising carrier for duloxetine hydrochloride with higher drug loading and greater pH-sensitive release.

Homopiperazine grafted mesoporous silicas from rice husk ash for CO2 adsorption.

Chloro-functionalized mesoporous MCM-41, SBA-15, MCM-48 and KIT-6 were synthesized by co-condensation of 3-chloropropyl-trimethoxy-silane (CPTMS) and rice husk ash sodium silicate solution, which is subsequently grafted with a heterocyclic amine, homopiperazine (HPZ). X-ray powder diffraction and BET analysis of the chloro-functionalized mesoporous silicas confirmed the similarity between their structural properties and those obtained from conventional silica sources. CO2 adsorption studies of all HPZ-grafted mesoporous silicas exhibited 8-10 wt% of adsorption capacity and are found to be selective, recyclable and thermally stable. Here, the CO2 adsorption reaction is via the traditional carbamate mechanism. The presence of both secondary and tertiary amine in HPZ influences the high CO2 adsorption capacity. Hence, these HPZ-grafted mesoporous silicas could contribute to CO2 capture as a green, tunable, selective and efficient sorbent.

Evaluation of antiviral and cytotoxic activities of methanolic extract of S. grandiflora (Fabaceae) flowers.

OBJECTIVE: To investigate the cytotoxicity and antiviral activity of methanolic extract of S. grandiflora flowers using different cell lines and viruses. METHODS: The methanolic flower extracts were prepared and evaluated for their antiviral and cytotoxic activities using viruses like herpes simplex-1 and 2, vaccinia, vesicular stomatitis, cox sackie, respiratory syncytical, feline corona, feline herpes, para influenza, reo-1, sindbis and punta toro viruses in different cell lines, like Hel, HeLa, Crandell Reus feline kidney and Vero cell cultures. RESULTS: Among the viruses used the extract possessed strongest antiviral activity against herpes simplex 1 and 2, repiratory syncytical, para influenza, reo, sindbis, cox sackie and punta toro viruses that was (EC50=20 µg/mL and 45 µg/mL) and moderate activity for remaining viruses (EC50= 100 µg/mL). The antiviral activities assessed by calculating the selectivity index may be due to the presence of flavonoids in the extracts there by inhibit the virus cell fusion in the early and replication stages. The cytotoxicity effect was evaluated using MTT assay and the results revealed that the extracts exhibited cytotoxicity from the range of 20 to 100 µg/mL. CONCLUSIONS: Present results confirmed that the S. grandiflora used as a good antimicrobial agent in future.

Evaluation of antiviral and cytotoxic activities of methanolic extract of S. grandiflora (Fabaceae) flowers

Objective: To investigate the cytotoxicity and antiviral activity of methanolic extract of S.grandiflora flowers using different cell lines and viruses. Methods: The methanolic flower extracts were prepared and evaluated for their antiviral and cytotoxic activities using viruses like herpes simplex-1 and 2, vaccinia, vesicular stomatitis, cox sackie, respiratory syncytical, feline corona, feline herpes, para influenza, reo-1, sindbis and punta toro viruses in different cell lines, like Hel, HeLa, Crandell Reus feline kidney and Vero cell cultures. Results: Among the viruses used the extract possessed strongest antiviral activity against herpes simplex 1 and 2, repiratory syncytical, para influenza, reo, sindbis, cox sackie and punta toro viruses that was (EC50=20 μg/mL and 45 μg/mL) and moderate activity for remaining viruses (EC50= 100 μg/mL). The antiviral activities assessed by calculating the selectivity index may be due to the presence of flavonoids in the extracts there by inhibit the virus cell fusion in the early and replication stages. The cytotoxicity effect was evaluated using MTT assay and the results revealed that the extracts exhibited cytotoxicity from the range of 20 to 100 μg/mL. Conclusions: Present results confirmed that the S. grandiflora used as a good antimicrobial agent in future.

Quantitation of alfuzosin hydrochloride in pharmaceutical formulations by RP-HPLC.

An isocratic reversed phase high-performance liquid chromatographic (HPLC) method with ultraviolet detection at 245 nm has been developed for the determination of alfuzosin hydrochloride in dosage formulation. Good chromatographic separation alfuzosin was achieved by using a stainless steel analytical column Inertsil ODS-3V (5 microm, 15 cmx0.46 cm). The system was operated at ambient temperature (25+/-2 C) using a mobile phase consisting of acetonitrile:water:tetrahydrofuran:perchloricacid (250:740:10:1) at a flow rate of 1 ml/min. The calibration curve for alfuzosin hydrochloride was linear over the tested concentration range of 50%, 75%, 100%, 125% and 150% with reference to the label claim and a correlation coefficient of 0.999. The intra- and inter-run precision and accuracy results were 98.07 to 100.34 with the %RSD of 0.71% and tailings factor 1.07. The proposed method was validated for its selectivity, linearity, accuracy, and precision. The method was found to be suitable for the quality control of alfuzosin hydrochloride in bulk drug as well as in formulation.