pH Responsive Polymeric Nanoparticles for Oral Insulin Delivery

Gelatin-eudragit L100 nanoparticles of wet size range 170-563nm were prepared by two step dissolvation method and the effect of different concentrations of eudragit L100 and emulsifying agent - sodium lauryl sulphate (SLS) - on the particle size were studied. Synthesized nanoparticles were characterized by attenuated total reflectance-fourier transform infrared spectroscopy (ATRFTIR) and the mean size distribution. Insulin loading was done at a pH 7.4 and the in vitro insulin release studies of nanoparticles were carried out by simulating gastrointestinal tract condition which showed the minimal insulin release at pH 2.5 (20% in 90min) while appreciable release (40% in first 30min) at pH of 7.4. This pH responsive release pattern of the synthesized nanoparticles confers on the insulin protection from proteolytic degradation in acidic environment of stomach and upper intestinal part while enhancing bioavailability in the later part of intestine.

Reversal of reserpine-induced orofacial dyskinesia and catalepsy by Sida cordifolia

Reserpine-induced catalepsy is an animal model used to mimic the behavioural symptoms of Parkinson’s disease (PD) in experimental animals. The present study was designed to investigate the effect of aqueous and hydro-ethanolic extracts of Sida cordifolia (AESC and EESC respectively), in reserpine-induced orofacial dyskinesia and catalepsy along with lipid peroxidation evaluated by the levels of thiobarbituric acid like reactive substances (TBARS) in rat forebrain. Sida cordifolia is a well know Ayurvedic plant which has been administered anciently for nervous disorders such as hemiplegia, facial paralysis and PD. It also possesses significant in vitro and ex vivo antioxidant activity. Repeated administration of reserpine (1 mg/kg; s.c.) on alternate days (day 1, 3 and 5) for a period of 5 days significantly increased the vacuous chewing movements (VCM), tongue protrusions (TP), orofacial bursts (OB) and catalepsy along with increased forebrain TBARS levels in rats which was dose-dependently reversed by AESC (50, 100 and 250 mg/kg; p.o.) treatment. No significant effect on these behavioural parameters was observed following varying dose (50, 100 and 250 mg/kg; p.o.) treatment of EESC in reserpine treated rats. These findings suggest the involvement of antioxidant activity along with other underlying mechanisms for the ameliorative effect of AESC in reserpine-induced orofacial dyskinesia and catalepsy. It predicts the scope of AESC in the possible treatment of neuroleptic-induced orofacial dyskinesia and PD

A Prospective Comparative Study of serratiopeptidase and aceclofenac in Upper and Lower Limb Soft Tissue Trauma Cases

The aim of this study was to evaluate and compare the efficacy and safety of serratiopeptidase and aceclofenac in reducing swelling and pain following soft tissue injury. This study included 100 patients with soft tissue injury to upper limb, lower limb or both. They were randomly divided into two groups of 50 each to receive serratiopeptidase and aceclofenac. Evaluation of efficacy was made using tape measurement (for swelling), and visual analogue scale (for pain) on day 0, week 1and week 2. Serratiopeptidase showed significant anti-inflammatory effect and mild analgesic effect. None of the patient was required to be put on another analgesic or any alteration in treatment. Aceclofenac showed superior analgesic effect as compared to serratiopeptidase. Mild to moderate adverse effects were reported. The most common adverse effect reported was dyspepsia. All were mild and did not require any alteration or discontinuation of treatment.

Hepatoprotective Effect of Carrot (Daucus carota L.) on Paracetamol Intoxicated Rats

Plant products play a crucial role in the hepatoprotection through its antioxidants property. Therefore, search for modern medicine of plant origin with this property has become a central focus on hepatoprotection today. This study investigated to search a new hepatoprotective agent from natural sources, the methanol extract of nutitional plant, Daucus carota leaves was tested against liver damage of albino rats. Levels of serum marker enzymes i.e. SGOT, SGPT (aminotransferases), ALP (alkaline phosphatase) and TB (total bilirubin) in serum respectively. The histopathological changes of liver sections were also compared with the respective controls. 30% paracetamol induced significant (P<0.05) increase in liver enzymes alongwith the hepatic necrosis and other visible disarrangements in hepatic tissues. Simultaneously, oral treatment with kaempferol (KF) isolated from D. carota plant reversed to all the serum and liver parameters, dose-dependently, in 30% paracetamol treated rats. The biochemical results were also compared with the standard drug i.e. silymarin. These findings indicate the hepatoprotective potential of D. carota fruit against liver damage might be due to the presence of flavonoid like KF constituents.

PHYSICO-CHEMICAL AND PHYTO-CHEMICAL STUDY OF RHIZOME of Cyperus rotundus LINN

Cyperus rotundus L., (Family Cyperaceae), also known as purple nutsedge or nutgrass, is a common perennial plant. This is a multipurpose plant, widely used in traditional medicine around the world to treat various diseases such as indigestion, constipation, dysentery, abdominal distention, neurogenic gastralgia, chest pains, irregular menstruation, painful menstruation, skin diseases, furuncle infections, leprosy, sprains and bruises, and fever. It has the property of therapeutic actions such as analgesic, alternative, astringent, antispasmodic, antibacterial, carminative, contraceptive, demulcent, emmenagogue, emollient, febrifuge, immunostimulant, laxative, tonic, vermifuge. Pharmacognostical investigations are the first and foremost step to determine the identity and to assess the quality of plant species. The aim of the study was to evaluate the parameter to determine the quality of the rhizome of Cyperus rotundus L. These studies comprise to investigate macroscopy, microscopy, physicochemical parameters, preliminary phytochemical screening and fluorescence characteristics. The findings may provide useful information with regard to its identification and standardization in future.

Poly (PEGDMA-MAA) copolymeric micro and nanoparticles for oral insulin delivery : A molecular mechanistic revisit

Poly(ethylene glycol) dimethacrylate (PEGDMA) and methacrylic acid (MAA) based micro and nanoparticles were prepared for oral insulin delivery. The reactional profiles of MAA, PEGDMA and PEGDMA-MAA were elucidated using molecular mechanics energy relationships (MMER) in vacuum and in a solvated system by exploring the spatial disposition of different concentrations of polymers with respect to each other. Furthermore, the incorporation of insulin within the polymeric matrix was modeled using connolly molecular surfaces. The computational results corroborated with the experimental and analytical data. The ability to effectively control blood glucose level coupled with the non toxic behavior of the nanoparticles renders them a potential candidate for insulin delivery.

EVALUATION OF THE SUSPENDING PROPERTIES OF A NEW PLANT GUM IN SULPHAMETOXAZOLE FORMULATIONS

Suspension dosage forms require the use of suspending agents in order to deliver a uniform dose of the active ingredient. The purpose of this study is to investigate the properties of a new plant gum as a cheap and effective natural polymer in the formulation of pharmaceutical suspensions. The gum obtained from the incised trunk of Cedrela odorata (family Meliaceae) was compared with hydroxypropylmethylcellulose and gelatin in Sulphamethoxazole suspension formulations at concentrations of 1.0 – 4.0%w/w. Assessment parameters were sedimentation volume, flow rate, viscosity and the effect of temperature on these parameters. The suspending characteristics of Cedrela gum compared well with that of hydroxypropylmethylcellulose in term of sedimentation volume, flow rate and viscosity and the natural gum could be used as a substitute in pharmaceutical suspensions.

Antibacterial Remedies Based on the Flora of Northern Kazakhstan

It was developed by us a medicinal products line that includes components of Populus balsamifera L., Populus tremula L., Chelidonium majus L., Glycyrrhiza uralensis Fisch. The basis for the creation of the line was vegetative parts of balsam poplar. It was developed and patented a new method of obtaining biologically active substances from balsam poplar. It was determined the dynamics of changes in various indices of herbal raw material. The antiseptic tincture and suppositories on the base of substance were developed. Selected fraction of terpenoids uses as remedy and effectively fights all forms of lung tuberculosis pathogens, removes bacterial and fungal infection, helps to improve immunity, and forces the bronchus cure. An aerosol form of medication on the basis fraction of terpenoids is being developed. It is developed composition of the dosage form (syrup), which includes wartwort alkaloids, phenolic compounds of aspen, an extract of licorice, for the treatment of concomitant assident fungus and bacterial flora.

Assessment of In-vitro Wound Healing Activity of the Tinospora crispa Extracts

Wound healing is a complex and dynamic process which follows the normal physiology trajectory through the phases of homeostasis, inflammation, granulation and maturation. Malaysia has a rich collection of plant based healing. A large number of plants are used for the treatment of cuts and wounds by folklore traditions in Malaysia. Tinospora crispa Miers. (Menispermaceae) is popular in Asian countries for its miracle of curing diseases. T.crispa differs slightly from T.cordifolia which is well distributed in India. Considerable researches have reported the activity of this plant possessing anti-malarial, diabetes treatment etc. In Malaysia, it is used traditionally for wound healing. Hence, the present study was aimed to evaluate its scientific validity. Stems of the plant were air dried after reduced into smaller size. Dried stems were then crushed into coarse powder. Then it was introduced into methanolfor extraction by cold maceration technique. The extract was filteredafter 7 days andfractionatedwith addition of chloroform. The methanol and chloroform fractions were made to evaporate until concentrated and formulated into ointments.Albino rats were separated into four groups of six rats in each group.All four groups were divided and served as a control, methanol fraction, chloroform fraction and standard drug (Betadine) respectively. The methanol extract and chloroform extract were investigated for the evaluation of its healing efficiency on excision wound model in Albino rats. Woundclosure in percentage was used to evaluate the effect on wound healing.The methanol fraction and chloroform fraction showed a significant wound healing activity which was well comparable with the standard drug used. Methanol fraction ointment showed greater activity than chloroform fraction. This study indicated that the methanol fraction ointment possesses wound healing property which substantiates the folklore claim.

Synthesis and anticonvulsant activity of some 1-cyclohexylidine/ cycloheptylidine-4-substitued semicarbazide derivatives

Aryl semicarbazide derivatives are reported to possess anticonvulsant activity. On the other hand unsubstituted and small substituents (less than 3 carbon atom) containing cyclohexanones prevented both pentylenetetrazole and MES induced seizures. Similarly cycloheptanone fused with benzodiazepine and furan produced anticonvulsant compounds. Therefore looking into the above facts in the present study, we have synthesized 12 derivatives of 1-cyclohexylidine/cycloheptylidine-4-substitued semicarbazide derivatives and screened them for anticonvulsant activity. The synthesis of compounds was achieved as follows: The various para substituted (H, CH3, F,Cl,Br, I) anilines were converted to aryl ureas by reacting with sodium cyanate in the presence of glacial acetic acid. These aryl ureas and aryl semicarbazides were synthesized by allowing them to react with hydrazine hydrate. Finally the aryl semicarbazides were condensed with cyclohexanone/ cycloheptanone in the presence of sodium acetate to give title compounds. All the synthesized compounds were evaluated for anticonvulsant activity by MES method using carbamazepine as standard and it was observed that all the compounds possess anticonvulsant activity comparable to carbamazepine. Carbamazepine had shown the abolition in the hind limb extensor tonic convulsion after 2 sec. whereas few compounds i.e. 1-cyclohexylidine-4-(4-fluorophenyl) semicarbazide, 1-cycloheptylidine-4-(4- fluorophenyl) semi-carbazide and 1-cycloheptylidine-4-phenylsemicarbazide were more active than standard. Overall it was found that cycloheptyl containing compounds were more active than cyclohexyl containing compounds. The unsubstitued compounds were more active than halo derivatives i.e. electron withdrawing groups, and halo compounds were more active than methyl derivatives i.e. electron donating group (CH3). The order of activity for cyclohexanone and cycloheptanone derivatives is as follows: H >F >Cl >Br >I >CH3. Among the halo derivatives, the activity decreased with increasing molecular weight of halo substituents.