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Piroxicam loaded polymer hybrid microspheres based tablets with modified release kinetics: Development, characterization and in vivo evaluation

2022-10-24T11:24:55Z

Title: Piroxicam loaded polymer hybrid microspheres based tablets with modified release kinetics: Development, characterization and in vivo evaluation Authors: Hamid, Hajra Afeera; Khan, Shahzeb; Shah, Syed Muhammad Noor; Asghar, Muhammad; Shahid, Muhammad; Hussain, Zahid; Sohail, Muhammad; Barkat, Ali Khan; Amin, Fazli; Jan, Syed Umer; Elhissi, Abdelbary; Shah, Syed Muhammad Hassan; Minhas, Muhammad Usman; Shah, Syed Wadood Ali; Ahmad, Naveed Abstract: Piroxicam (PC) is a non-steroidal anti-inflammatory drug characterized by poor aqueous solubility and reported to cause and impart crucial GIT irritation, bleeding, peptic and duodenal ulcer. Engineering of PC loaded microcapsules and its surface modification using different polymers has become the popular approach to address the said issues. The purpose of the study was to develop new PC loaded gastro-protective polymer hybrid microspheres (PHM) with subsequent conversion to tablet dosage form having modified dissolution rate and improved bioavailability. The crystallinity of the PC loaded PHM were established through powder X-ray diffraction. The optimised microspheres, PCM1 with particle size 32±3.0µm, entrapment efficiency 83.78±2.5% and in vitro drug release 87.1±2.6% were further subjected to tablets development and in vivo evaluation. The in vitro drug release study conducted for PHM at pH media 1.2 and 6.8 demonstrated retarded and enhanced drug release rates (P<0.001) respectively. Both accelerated and real time stability studies confirmed stability of the PC loaded PHM based tablets. A substantial improvement in the drug plasma concentration 12.6±2.36 (P<0.001) was observed for the produced tablets compared to the marketed formulations.

Cardiotonic potential of Carissa opaca Stapf ex Haines: A study on isolated rabbit heart

2022-10-24T08:49:18Z

Title: Cardiotonic potential of Carissa opaca Stapf ex Haines: A study on isolated rabbit heart Authors: Alqahtani, Yahya S; Amir, Huma; Alamgeer; Ahmad, Taseer; Mahnashi, Mater H; Alyami, Bandar A; Alqarni, Ali O; Akram, Muhammad; Khan, Hafeez Ullah Abstract: : Carissa opaca (C.O) is a wild shrub, belonging to the family Apocynaceae. The medicinal virtues of this plant have long been known. The present study demonstrates the effects of aqueous-methanolic extract and various fractions (n-butanolic and aqueous) of Carissa opaca on cardiovascular parameters. The perfusion pressure (PP), force of contraction (FC) and heart rate (HR) were assessed on isolated heart of rabbit using Langendroff’s technique for crude extract and fractions of C.O, followed by the elucidation of the mechanism of action after estimating toxicity of the plant. Negative ionotropic and positive chronotropic effects, with an increase in PP in isolated perfused rabbit heart were observed the with plant extract and fractions. The aqueous-methanolic extract exhibited maximum response at 1mg/ml while the n-butanolic and aqueous fractions showed a maximum response at 1mg/ml and 10µg/ml respectively. Both fractions produced the same response when treated with atropine (10-5 M), however the actions of adrenaline (10-5 M) and calcium chloride (10-5 M) remained unblocked. Acute toxicity studies indicated that the plant was safe up to 2000 mg/kg and sub-chronic studies demonstrated that no significant change in haematological and biochemical parameters observed. In conclusion, this study supports the folkloric claim of C.O extract.

Cardioprotective effect of boswellic acids against doxorubicin induced myocardial infarction in rats

2022-10-24T08:48:30Z

Title: Cardioprotective effect of boswellic acids against doxorubicin induced myocardial infarction in rats Authors: Shahid, Muhammad Hassaan; Anjum, Irfan; Mushtaq, Muhammad Naveed; Riaz, Saba Abstract: The aim of the present study was to evaluate the cardioprotective activity of boswellic acids in doxorubicin (DOX) induced cardiotoxicity. DOX (2.5mg/kg) was used intraperitoneally in rats to induce cardiotoxicity in six divided doses every alternate day over a period of two weeks. Dexrazoxane (10:1) was used as a standard drug. Boswellic acids (250, 500 and 750 mg/kg) were orally administered to rats for 14 days. After 14 days, rats were sacrificed, and blood was withdrawn through cardiac puncture. The blood lipid profile and cardiac biomarkers including LDH, CK-MB, CPK, SGOT and troponin T were measured. The heart of rats was isolated for histopathological studies. Graphpad Prism was used for statistical analysis. There was a significant increase in the level of cardiac enzymes and complete lipid profile parameters in diseased group as compared to control group. Pre-treatment with boswellic acids decreased level of all the measured parameters and decreased the severity of myocardial damage as supported by histopathological studies. It was concluded that boswellic acids possess cardioprotective potential by lowering cardiac biomarkers and blood lipid profile. Thus, boswellic acids might act as cardioprotective agent against doxorubicin induced cardiotoxicity.

Synthesis and anticancer evaluation of 2-oxo-2-(arylamino) ethyl 4- phenylpiperazine-1-carbodithioates

2022-10-24T08:47:50Z

Title: Synthesis and anticancer evaluation of 2-oxo-2-(arylamino) ethyl 4- phenylpiperazine-1-carbodithioates Authors: Hafeez, Freeha; Zahoor, Ameer Fawad; Rasul, Azhar; Ahmad, Sajjad; Mansha, Asim Abstract: Piperazine moiety is found as an efficient pharmacological scaffold in various drugs. To explore the anticancer potential of piperazine framework, a series of novel N-acetamides derivatives of phenyl piperazine containing di-thio-carbamate moiety was designed and synthesized. 1HNMR, 13CNMR, FT-IR and mass spectrometry were used for the structures elucidation of these derivatives. In-vitro cytotoxic evaluation of the prepared novel compounds against lung carcinoma A-549 was carried out using standard MTT assay. All the di-thio-carbamate-piperazine derivatives exhibited moderate to excellent cytotoxic potential against A-549 cell line based on cell viability. Particularly, 6e was found to be the most potent derivative with cell viability 34.12±0.73 % at 100 µg/mL concentration and represents promising lead compound for future progress.