Preliminary pharmacological evaluation of Martynia annua Linn leaves for wound healing.

OBJECTIVE: To evaluate the wound healing potential of fractions from ethanol extract of Martynia annua (M. annua) Linn leaves. METHODS: Ethanol extract of M. annua Linn leaves was fractionate into three different fractions (MAF-A, MAF-B and MAF-C) which were screened for wound healing potential using two models: excision and incision on rats. The thin layer chromatography (TLC) profile of all fractions were analyzed and TLC of luteolin was also done. The Povidone-Iodine Ointment was used as reference for comparision. Excision and incision wounds were created on dorsal portion of rats for study. Wound contraction, biochemical parameters (protein level and hydroxyproline level) and histopathological study were performed in excision wound model whereas incision model was used for determination of tensile strength. RESULTS: The wound contraction and tensile strength of skin tissues were observed significantly greater in MAF-C fraction treated group than other two fractions (P<0.01). In excision wound method (on day 18) protein content and hydroxyproline were found significantly higher in MAF-C group than control group (P<0.01). Histopathological study also showed better angiogenesis, matured collagen fibres and fibroblast cells as compared with the control group. CONCLUSIONS: In conclusion, our findings suggest that fraction MAF-C from ethanol extract of M. annua leaves is found most effective in wound healing.

Nephroprotective activity of Momordica dioica Roxb. in cisplatin-induced nephrotoxicity.

In this study, the ethanol extract of Momordica dioica fruit extract (200 mg kg(-1)) was studied for nephroprotective and curative activities. Chloroform, ethyl acetate, ethanol and aqueous extracts were prepared. In vitro antioxidant activity was made the basis for the selection of the ethanol extract for further studies. In DPPH free radical scavenging activity, the ethanolic extract has shown maximum inhibition (84.2%), followed by aqueous (74.8%), ethyl acetate (69.4%) and chloroform (59.7%) extract. On the other hand, in total antioxidant activity, the ethanol extract has shown 80.1% inhibition, followed by aqueous (71.9%), ethyl acetate (67.2%) and chloroform (53.2%) extracts. A single dose (5 mg kg(-1), i.p.) of cisplatin was administrated to induce nephrotoxicity. Blood urea and serum creatinine were analysed as biochemical markers of nephrotoxicity. Reduced glutathione (GSH) and the product of lipid peroxidation (MDA) were also measured in kidney tissues. A single dose of cisplatin resulted in significant reduction in body weight and increased the urea and creatinine levels. Extract administration has shown significant recovery in the levels of these biochemicals in curative (p < 0.001) and protective groups, whereas a single dose of cisplatin caused significant reduction in GSH and an increase in malondialdehyde production. Recovery was observed in treated groups. This study suggested that the nephroprotective and curative activities of M. dioica fruit extract are due to its antioxidant activity. It is further concluded that this antioxidant activity may be attributed to the phenolics, flavonoids and amino acids present in the extract.

Design and optimization of floating drug delivery system of acyclovir.

The purpose of the present work was to design and optimize floating drug delivery systems of acyclovir using psyllium husk and hydroxypropylmethylcellulose K4M as the polymers and sodium bicarbonate as a gas generating agent. The tablets were prepared by wet granulation method. A 3(2) full factorial design was used for optimization of drug release profile. The amount of psyllium husk (X1) and hydroxypropylmethylcellulose K4M (X2) were selected as independent variables. The times required for 50% (t(50%)) and 70% (t(70%)) drug dissolution were selected as dependent variables. All the designed nine batches of formulations were evaluated for hardness, friability, weight variation, drug content uniformity, swelling index, in vitro buoyancy, and in vitro drug release profile. All formulations had floating lag time below 3 min and constantly floated on dissolution medium for more than 24 h. Validity of the developed polynomial equation was verified by designing two check point formulations (C1 and C2). The closeness of predicted and observed values for t(50%) and t(70%) indicates validity of derived equations for the dependent variables. These studies indicated that the proper balance between psyllium husk and hydroxypropylmethylcellulose K4M can produce a drug dissolution profile similar to the predicted dissolution profile. The optimized formulations followed Higuchi's kinetics while the drug release mechanism was found to be anomalous type, controlled by diffusion through the swollen matrix.

Effect of Momordica dioica Roxb on gentamicin model of acute renal failure.

The ethanolic extract of the fruits of Momordica dioica was studied for its protective and curative effect against gentamicin-induced acute renal injury in albino rats of both sexes. Gentamicin intoxicated group showed significant increase in blood urea (69.48 +/- 4.34) and serum creatinine (3.017 +/- 0.208) from normal levels 33.72 +/- 1.92 and 0.818 +/- 0.073, respectively, in control group. In the preventive regimen, the extract at dose levels of 200 mg kg(-1) showed significant reduction in the elevated blood urea (47.93 +/- 2.46) and serum creatinine (2.067 +/- 0.1745), respectively. This treatment normalised the histopathological changes compared to the intoxicated group. In the curative regimen at 200 mg kg(-1) blood urea was found to be 48.21 +/- 2.36 and serum creatinine level was 2.050 +/- 0.183, which revealed significant curative effect. In vivo antioxidant and free radial scavenging activities were also determined. The maximum free radical scavenging activity with ethanolic extract was the basis of selection of this extract for in vivo study. Reduced glutathione (GSH) level was significantly (p < 0.05) increased in the extract treated groups whereas malondialdehyde (MDA) was reduced significantly (p < 0.05). High content of flavonoids and phenolic compounds was found in ethanolic extract, which may be responsible for free radical activity. The findings suggest that the ethanol extract of Momordica dioica seeds possesses marked nephroprotective and curative activities without any toxicity due to its antioxidant activity and could offer a promising role in the treatment of acute renal injury caused by nephrotoxin-like gentamicin.

Role of chelates in treatment of cancer.

Chelates are used in cancer as cytotoxic agent, as radioactive agent in imaging studies and in radioimmunotherapy. Various chelates based on ruthenium, copper, zinc organocobalt, gold, platinum, palladium, cobalt, nickel and iron are reported as cytotoxic agent. Monoclonal antibodies labeled with radioactive metals such as yttrium-90, indium-111 and iodine-131 are used in radioimmunotherapy. This review is an attempt to compile the use of chelates as cytotoxic drugs and in radioimmunotherapy.

Wound healing potential of Tephrosia purpurea (Linn.) Pers. in rats.

Tephrosia purpurea is a well-known herb for its hepatoprotective, anticancer, antiulcer, antibacterial and in healing bleeding piles, etc. The present study was aimed for wound healing potential of ethanolic extract of Tephrosia purpurea (aerial part) in the form of simple ointment using three types of wound models in rats as incision wound, excision wound and dead space wound. The results were comparable to standard drug Fluticasone propionate ointment, in terms of wound contraction, tensile strength, histopathological and biochemical parameters such as hydroxyproline content, protein level, etc. Histopathological study showed significant (P<0.05) increase in fibroblast cells, collagen fibres and blood vessels formation. All parameters were observed significant (P<0.05) in comparison to control group.

Antimicrobial activity of the roots of cocculus hirsutus.

Cocculus hirsutus Linn was studied for antimicrobial activity against Staphylococcus aureus, Echerchia coli, Pseudomonas aeruginosa and Salmonella typhi using agar disc-diffusion method. Petroleum ether extract, Ethanolic extract and Crude alkaloidal fraction were screened for the activity in various concentrations and zone of inhibitions were recorded. Results suggest that the Ethanolic extract and Crude alkaloidal fraction have significant antimicrobial activity against test microorganisms and the activity is found to be concentration dependent. Present findings justify the claimed uses of Cocculus hirsutus in the indigenous systems of medicine to treat various infectious diseases.

Analgesic activity of the roots of baliospormum montanum linn.

The ethanolic extract and its chloroform soluble and chloroform insoluble fractions of the roots of Baliospermum montanum were investigated in albino rats to evaluate the analgesic activity. Tailo - flick animal model was employed to test analgesic activity and compaired with a standard drug, Diclofenac sodium. The results indicate that the ethanolic extract and its chloroform soluble fraction are significantly effective (p<0.05) with respect to standard. The activity was found to be dose dependant. Results of present study justify the folklore use of B.montanum as analgesic drug.

Evaluation of an aqueous injection of ketoprofen.

The increase in aqueous solubility of ketoprofen using hydrotropes and cosolvents in formulation, as well as stability studies of its aqueous injections have been reported earlier. These formulations were further evaluated in vitro (physical evaluation, haemolytic activity) and in vivo (pharmacokinetic studies). Some of the formulations have shown promising results.

Cosolvent solubilization and formulation of an aqueous injection of ketoprofen.

Ketoprofen (1) an analgesic, antipyretic and anti-inflammatory agent, is practically insoluble in water. An increase in the aqueous solubility of 1 was attempted by various cosolvents. The solubility increased up to 8556 times (maximum) in case of ethanol while it was 33 times (minimum) in case of glycerol. Using selected cosolvents and hydrotropes, aqueous injections of 1 were formulated.