To establish quality control parameters of a locally occurring medicinal plant, Malva parviflora which is utilized as folk medicine in Sialkot area in Pakistan. In pharmacognostic studies different types of evaluations were carried out that focus on microscopic, macroscopic, fluorescence analysis and organoleptic evaluations. The distinguishing characters of stem were the presence of parenchyma, cork cells, irregular shape calcium oxalate crystals, simple and compound starch granules and fusiform fibers with pits. Root microscopic characters were presence of simple and spherical starch granules with rounded or slit hilum, groups of lignified xylem fibers, reticulate vessels, and sieve tissues. Leaves microscopy indicated the presence of paracytic stomata, lignified fibers having pits, spiral and annular vessels, numerous sclereids while in fruit microscopy epicarp, thin walled cells endocarp, thin walled parenchyma and collenchyma of mesocarp and abundant thick walled endospermic cells containing aleurone grains and micro rosette crystals. Macroscopic study of leaves showed, 5-7 lobed reniform-shape, glabrous-surface, reticulate-venation in the leaves. Macroscopic features of roots showed type of root-taproot, surface-glabrous and stem was 1-10 dm tall simple to branched and may be prostrate or ascending. Similarly fruit was of schizocarp type. This study provides the scientific data for the proper identification and establishment of standards for the use of Malva parviflora.
The objective of the current study was to achieve a sustained release profile of capecitabine (CAP), an anticancer agent frequently administered in conventional dosage form due to its short plasma half-life. A drug-loaded smart pH responsive chitosan/fenugreek-g-poly (MAA) hydrogel was synthesized by an aqueous free radical polymerization technique. The developed network was evaluated for capecitabine loading %, swelling response, morphology, structural and compositional characteristics, and drug release behavior. Significantly higher swelling and in vitro drug release rate were exhibited by formulations at pH 7.4 than at pH 1.2, demonstrating the pH responsive character of hydrogels. Swelling percentage and CAP loading ranged within 74.45–83.54% and 50.13–72.43%, respectively. Maximum release, up to 93%, was demonstrated over 30 h, evidencing the controlled release pattern of CAP from hydrogels. The optimized formulation was further screened for acute oral toxicity studies. No signs of oral, dermal, or ocular toxicities were noticed, confirming safety evidence of the network. Furthermore, pharmacokinetic analysis demonstrated the sustained release response of CAP from hydrogels as confirmed by a significant increase in plasma half-life (t1/2) (13 h) and AUC (42.88 µg h/mL) of CAP. Based on these findings, fabricated hydrogels are strongly recommended as a biocompatible carrier for colorectal delivery of active agents.
1 September 2014 in Asian Pacific Journal of Tropical Medicine
To evaluate the phytochemical and in vitro antioxidant ability of methanolic extract and different fractions of Amaranthus graecizans subsp. silvestris (A. graecizans subsp. silvestris). Methanolic extract of A. graecizans subsp. silvestris was obtained by cold maceration and then methanolic extract was subjected to fractionation and different fractions i.e. n-hexane, chloroform, ethyl acetate, n-butanol and aqueous fractions were obtained. Methanolic extract and all other fractions were subjected to phytochemical investigation by performing different phytochemical group tests like alkaloid, tannins, carbohydrates, lipids, proteins, etc. In vitro antioxidant activity of A. graecizans subsp. silvestris was evaluated by using 1, 1-diphenyl-2-picrylhydrazyl radical (DPPH), ferric thiocyanate assay, total antioxidant activity by phosphomolybdenum, ferric reducing antioxidant power, total phenolic content and lipid peroxidation methods. Maximum antioxidant activity was shown by n-hexane fraction of the extract by carrying out DPPH (86.44±0.23), ethyl acetate fraction by total antioxidant (0.95±0.06) and ferric reducing antioxidant power (299.45±1.48) methods, while by employing total phenolic contents and inhibition of lipid per oxidation assays, methanolic extract (92.88±4.16) and n-hexane fraction (69.47±0.68) exhibited maximal activity. Ethyl acetate fraction showed the least IC50 values by DPPH assay, hence a more pronounced potential for antioxidant activity. The results indicate that A. graecizans subsp. silvestris has antioxidant potential and can be utilized as a natural source of antioxidant.
In the present study, pH-sensitive, biodegradable, and biocompatible Na-CMC/pectin poly(methacrylic acid) hydrogels were synthesized using an aqueous free radical polymerization technique and encapsulated by cytarabine (anti-cancer drug). The aim of the project was to sustain the plasma profile of cytarabine through oral administration. Sodium carboxymethyl cellulose (Na-CMC) and pectin were cross-linked chemically with methacrylic acid (MAA) as a monomer, using methylene bisacrylamide (MBA) as cross-linker and ammonium per sulfate (APS) as an initiator. Prepared hydrogel formulations were characterized for their texture, morphology, cytarabine loading efficiency, compositional and structural properties, thermal nature, stability, swelling response, drug release profile (pH 1.2 and pH 7.4), and in-vivo pharmacokinetic evaluation. Cytarabine-loaded hydrogels were also evaluated for their safety profile by carrying out toxicity studies in rabbits. Results demonstrated efficient encapsulation of cytarabine into the prepared network with loading ranging from 48.5–82.3%. The highest swelling ratio of 39.38 and maximum drug release of 83.29–85.27% were observed at pH 7.4, highlighting the pH responsiveness of the grafted system. Furthermore, cytarabine maximum release was noticed over 24 h, ensuring a sustained release response for all formulations. Histopathological studies and hemolytic profiles confirmed that the prepared hydrogel system was safe, biocompatible, and non-irritant, showing no symptoms of any toxicities and degeneration in organs. Moreover, pharmacokinetic estimation of the cytarabine-loaded hydrogel showed a remarkable increase in the plasma half-life from 4.44 h to 9.24 h and AUC from 22.06 μg/mL.h to 56.94 μg/mL.h. This study revealed that the prepared hydrogel carrier system has excellent abilities in delivering the therapeutic moieties in a controlled manner.
Tofacitinib is an antirheumatic drug characterized by a short half-life and poor permeability, which necessitates the development of sustained release formulation with enhanced permeability potential. To achieve this goal, the free radical polymerization technique was employed to develop mucin/chitosan copolymer methacrylic acid (MU-CHI-Co-Poly (MAA))-based hydrogel microparticles. The developed hydrogel microparticles were characterized for EDX, FTIR, DSC, TGA, X-ray diffraction, SEM, drug loading; equilibrium swelling (%), in vitro drug release, sol–gel (%) studies, size and zeta potential, permeation, anti-arthritic activities, and acute oral toxicity studies. FTIR studies revealed the incorporation of the ingredients into the polymeric network, while EDX studies depicted the successful loading of tofacitinib into the network. The thermal analysis confirmed the heat stability of the system. SEM analysis displayed the porous structure of the hydrogels. Gel fraction showed an increasing tendency (74–98%) upon increasing the concentrations of the formulation ingredients. Formulations coated with Eudragit (2% w/w) and sodium lauryl sulfate (1% w/v) showed increased permeability. The formulations equilibrium swelling (%) increased (78–93%) at pH 7.4. Maximum drug loading and release (%) of (55.62–80.52%) and (78.02–90.56%), respectively, were noticed at pH 7.4, where the developed microparticles followed zero-order kinetics with case II transport. Anti-inflammatory studies revealed a significant dose-dependent decrease in paw edema in the rats. Oral toxicity studies confirmed the biocompatibility and non-toxicity of the formulated network. Thus, the developed pH-responsive hydrogel microparticles seem to have the potential to enhance permeability and control the delivery of tofacitinib for the management of rheumatoid arthritis.
4 August 2017 in BMC Complementary and Alternative Medicine
Herbology is the prevailing system among the nationally-accepted alternative or complementary systems of medicine. The system is due to its general and patient-oriented methodology, is widely used in the general population exposing them to the risk of the side effects of the herbal medicines. The aim of study was to assess the acute and sub-acute toxicity of the polyherbal formulation Hab-e-Kabad Noshadri tablets. In the acute arm of the study, a single dose of 2000 mg/kg was administered to Swiss Albino mice which were observed for physical symptoms and behavioral changes for 72 h. In sub-acute toxicity study repeated doses of the polyherbal preparation was administered to Wistar rats of both genders, separately. The animals received three doses of polyherbal product (50 mg/kg/day, 100 mg/kg/day and 200 mg/kg/day) for a period of 28 days. On 28th day of experiment, blood sampling of animals was done for hematological and biochemical analysis i.e. liver and renal function parameters, lipid profile and then sacrificed for histopathological examination of liver and kidney. There was no morbidity and mortality noticed with single dose administration in acute toxicity study in mice. In sub-acute toxicity study, morphological changes with some damage in liver and kidney tissues of male and female animals were recorded at dose of 100 mg/kg/day and 200 mg/kg/day. It was found that prolonged use at higher dose i.e. 200 mg/kg/day of this polyherbal formulation should be avoided and practitioners should cautiously prescribe this formulation in patients with hepatic and renal impairment.