Background The aim of the present study was to enhance the solubility of piroxicam (BCS class II drug) using co-crystallization technique and formulate the buccal films of selected co-crystals for improved therapeutic utilization of drug. Co-crystals of drug with various co-formers (molar ratio 1:1) were prepared by solvent evaporation method and were screened for their aqueous solubility and percent drug content. The formation of co-crystals was confirmed by FTIR, DSC and XRD. Piroxicam co-crystals loaded buccal films were prepared and evaluated for in vitro drug release, ex vivo drug permeation while safety of formulation was determined by histopathological study. Results The co-crystals prepared with different co-formers have proved their potential to improve the solubility of the drug. Co-crystals of piroxicam-sucralose have shown six-folds more solubility than parent drug. FTIR analysis indicated shifting in characteristics peaks of piroxicam. DSC analysis showed an extra exothermic peak and alteration in characteristic endothermic peak. The powder x-ray diffraction pattern exhibited changes in 2θ values of intense peaks. Thus, formation of co-crystal was confirmed. Physical characters of buccal films were found to be within limits. Formulation F6 showed highest mucoadhesive strength (5617 ± 636 dynes /cm2) while formulation F2 showed highest in vitro drug release after 8 h, i.e., 94.557%. The ex vivo drug permeation of F2 was found to be 84.74%. The hisopathological study revealed that there was no damage to buccal mucosal tissue and was found to be intact. Conclusion The piroxicam-suralose co-crystals based mucoadhesive films of piroxicam could be a better formulation approach with improved solubility, safety, and therapeutic efficacy as compared to conventional tablets. Graphical abstract

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Ipomoea reniformis Chaos is claimed in Indian traditional medical practice to be useful in the treatment of epilepsy and neurological disorders. In the present study, pretreatment effect of methanolic extract of Ipomoea reniformis on epilepsy and psychosis was evaluated in rodents using standard procedures. Besides evaluating epileptic and behavioral parameters, neurotransmitters such as Gamma-Amino Butyric Acid (GABA) in epilepsy and in psychosis dopamine, noradrenaline and serotonin contents in the rodent brain were estimated. The extract pretreatment reduced maximal electro shock; Isoniazid (INH) and Pentylenetetrazole (PTZ) induced seizures and also significantly inhibited the attenuation of brain GABA levels by INH and PTZ in mice. These results suggested that the observed beneficial effect in epilepsy may be by enhancing the GABAergic system. The test drug also inhibited the apomorphine induced climbing and stereotyped behavior and showed significantly reduced levels of brain dopamine, noradrenaline and serotonin which may be due to blocking of central dopaminergic, noradrenergic and serotonergic pathways or by enhancing the GABAergic system. The results obtained in present study suggest that the title plant possesses antiepileptic and antipsychotic activities in rodents.

Objective:Aim of this study is to evaluate antiurolithiatic potential of whole plant hydro-alcoholic (30:70) extract of Vernonia cinerea Less. in accordance to its claims made in ancient literature and also being one of the ingredients of cystone, a marketed formulation widely used in the management of urolithiasis.Materials and Methods:To induce urolithiasis, 0.75% v/v ethylene glycol was administered orally for 14 days. The curative dose of 400 mg/kg b.w. and preventive doses of 100, 200, and 400 mg/kg b.w. were administered from 15th to 28th and 1st to 28 days, respectively. Cystone 750 mg/kg b.w. was selected as the reference standard for both curative and preventive doses. On 28th day, urinate of 24 h was collected and subjected for estimation of calcium, oxalate, and phosphates. Serum biochemical and kidney homogenate analysis was done for determination of renal oxalate contents.Results:The diseased Group II showed marked increase (P < 0.001 vs. normal Group I) in levels of urine calcium, oxalate, and phosphate. Serum creatinine, urea, and uric acid levels were also increased. Histopathological studies of kidney sections revealed significant changes. Treatment with hydro-alcoholic extract of V. cinerea showed significant (P < 0.01 vs. calculi-induced Group II) dose-dependent activity. A progressive increase in urine output, body weight, and decline in concentrations of stone-forming components such as calcium, oxalates, and phosphates was observed.Conclusion:It can be inferred that V. cinerea Less. is effective in ethylene glycol-induced urolithiasis and may have a potential in preventing and curing urolithiasis.

Objectives: The present study deals with an in-vitro screening for the anti-solar potential of aqueous and ethanolic extracts of Cassia auriculata using the UV method. Methods: Aqueous and ethanolic extracts were prepared. Thus, prepared extracts were subjected to phytochemical investigation and evaluated for antioxidant effect using DPPH and antisolar efficacy. Concentrations ranging from 7.8 to 1000 μg/mL (serial dilution) were used for the determination of radical scavenging effect and concentration of 2 mg/mL was used for screening of anti-solar potential using Shimadzu UV-1700 double beam UV-Visible spectrophotometer. Readings were recorded in triplicate and graphs were extrapolated. Results: Extracts revealed the presence of important phytoconstituents such as phenols, triterpenoids, flavonoids, tannins, saponins, phytosterols, alkaloids and glycosides. Further, it was observed that Cassia auriculata possesses remarkable antioxidant activity. Significant results of the anti-solar screening study confirm its use as a natural sunscreen. It showed a protective effect against carcinogenic UV radiation. Ethanolic extract was found to be more effective in comparison with aqueous extract. Conclusion: From the data, it can be concluded that aqueous and ethanolic extracts showed promising antioxidant and anti-solar activity which could be considered as a rational alternative to chemically prepared synthetic sunscreen formulations available in the market.