Sanjay Kumar Jain

Dendrimer-mediated transdermal delivery: enhanced bioavailability of indomethacin

The transdermal delivery of aqueous formulations of indomethacin, a model drug, with different concentrations of three types of dendrimer showed a linear increase in flux with increasing concentration of each of the dendrimers. This result was in contrast to phase solubility studies, where Higuchis A(N) profile was observed. The steady-state flux of the drug increased significantly and was highest with the G4-NH2 dendrimer at 0.2% w/v concentration, which showed an enhancement factor of 4.5 compared to the pure drug suspension. In vivo, a steady-state flux was achieved in 5 h, and the C(max) values were significantly higher with G4-NH2 and G4-OH dendrimer formulations. The [AUC](0-24h) of G4-NH2 (2.27 times) and G4-OH (1.95 times) formulations were significantly higher than that of the pure drug, but was only marginally higher in the case of G-4.5 dendrimer formulation. The % inhibition of paw volume showed a trend comparable to the pharmacokinetic data and a maximum of 1.6- and 1.5-fold increase was found with G4-NH2 and G4-OH formulations, respectively, compared to the pure drug suspension.

Herbal antioxidant in clinical practice: a review.

Antioxidant-the word itself is magic. Using the antioxidant concept as a spearhead in proposed mechanisms for staving off so-called free-radical reactions, the rush is on to mine claims for the latest and most effective combination of free-radical scavenging compounds. We must acknowledge that such radicals have definitively been shown to damage all biochemical components such as DNA/RNA, carbohydrates, unsaturated lipids, proteins, and micronutrients such as carotenoids (alpha and beta carotene, lycopene), vitamins A, B6, B12, and folate. Defense strategies against such aggressive radical species include enzymes, antioxidants that occur naturally in the body (glutathione, uric acid, ubiquinol-10, and others) and radical scavenging nutrients, such as vitamins A, C, and E, and carotenoids. This paper will present a brief discussion of some well- and little-known herbs that may add to the optimization of antioxidant status and therefore offer added preventive values for overall health. It is important to state at the outset that antioxidants vary widely in their free-radical quenching effects and each may be individually attracted to specific cell sites. Further evidence of the specialized nature of the carotenoids is demonstrated by the appearance of two carotenoids in the macula region of the retina where beta-carotene is totally absent.

Plant profile, phytochemistry and pharmacology of Asparagus racemosus (Shatavari): A review.

Asparagus racemosus (A. racemosus) belongs to family Liliaceae and commonly known as Satawar, Satamuli, Satavari found at low altitudes throughout India. The dried roots of the plant are used as drug. The roots are said to be tonic and diuretic and galactgogue, the drug has ulcer healing effect probably via strenthening the mucosal resistance or cytoprotection. It has also been identified as one of the drugs to control the symotoms of AIDS. A. racemosus has also been successfully by some Ayurvedic practitioner for nervous disorder, inflammation and certain infectious disease. However, no scintific proof justify aborementioned uses of root extract of A. racemosus is available so far. Recently few reports are available demonstrating beneficial effects of alcoholic and water extract of the roots of A. racemosus in some clinical conditions and experimentally indused disease e.g. galactogougue affects, antihepatotoxic, immunomodulatory effects, immunoadjuvant effect, antilithiatic effect and teratogenicity of A. racemosus. The present artical includes the detailed exploration of pharmacological properties of the root extract of A. racemosus reported so far.

Pathophysiology of kidney, gallbladder and urinary stones treatment with herbal and allopathic medicine: A review

Medicinal plants have been known for millennia and are highly esteemed all over the world as a rich source of therapeutic agents for the prevention of various ailments. Today large number of population suffers from kidney stone, gall stone and urinary calculi. Stone disease has gained increasing significance due to changes in living conditions i.e. industrialization and malnutrition. Changes in prevalence and incidence, the occurrence of stone types and stone location, and the manner of stone removal are explained. Medicinal plants are used from centuries due to its safety, efficacy, cultural acceptability and lesser side effects as compared to synthetic drugs. The present article deals with measures to be adopted for the potential of medicinal plants in stone dissolving activity. The problem of urinary stones or calculi is a very ancient one and many remedies have been employed during the ages these stones are found in all parts of the urinary tract, the kidney, the ureters and the urinary bladder and may vary considerably in size. In the present article, an attempt has been made to emphasis on herbal option for urinary stone.

An update on Ayurvedic herb Convolvulus pluricaulis Choisy

Convolvulus pluricaulis Choisy (C. pluricaulis) is a perennial herb that seems like morning glory. All parts of the herb are known to possess therapeutic benefits. The plant is used locally in Indian and Chinese medicine to cure various diseases. It is used in Ayurvedic formulation for chronic cough, sleeplessness, epilepsy, hallucinations, anxiety etc. Based on the comprehensive review of plant profile, pharmacognosy, phytochemistry, pharmacological and toxicological data on the C. pluricaulis, there will be more opportunities for the future research and development on the herb C. pluricaulis. Information on the C. pluricaulis was collected via electronic search (using Pub Med, SciFinder, Google Scholar and Web of Science) and library search for articles published in peer-reviewed journals. Furthermore, information also was obtained from some local books on ethnopharmacology. This paper covers the literature, primarily pharmacological, from 1985 to the end of 2012. The C. pluricaulis is an important indigenous medicine, which has a long medicinal application for liver disease, epileptic disease, microbial disease, cytotoxic and viral diseases, central nervous system (CNS) disease in Ayurvedic medicine, traditional Chinese medicine and other indigenous medical systems. The isolated metabolites and crude extract have exhibited a wide of in vitro and in vivo pharmacological effect, including CNS depression, anxiolytic, tranquillizing, antidepressant, antistress, neurodegenerative, antiamnesic, antioxidant, hypolipidemic, immunomodulatory, analgesic, antifungal, antibacterial, antidiabetic, antiulcer, anticatatonic, and cardiovascular activity. A chemical study of this plant was then initiated, which led to the isolation of carbohydrats, proteins, alkaloids, fatty acids, steroids, coumarins, flavanoids, and glycosides as active chemicals that bring about its biological effects. A series of pharmacognostical studies of this plant show that it is a herb, its stem and leaves are hairy, more over it has two types of stomata, anisocytic and paracytic. A herb, C. pluricaulis has emerged as a good source of the traditional medicine for the treatment of liver disease, epileptic disease, microbial disease, cytotoxic and viral diseases, and CNS disease. Pharmacological results have validated the use of this species in traditional medicine. All the parts of the herb are known to possess therapeutic benefits. Expansion of research materials would provide more opportunities for the discovery of new bioactive principles from C. pluricaulis.

Poly (amidoamine) dendrimer-mediated hybrid formulation for combination therapy of ramipril and hydrochlorothiazide

&NA; We present a dendrimer‐based hybrid formulation strategy to explore the potential of poly (amidoamine) PAMAM dendrimers to be used as drug carriers for combination therapy of an anti‐hypertensive drug ramipril (RAPL) and a diuretic hydrochlorothiazide (HCTZ). The drug‐dendrimer complexes were prepared by phase‐equilibration method. The results showed that the solubility of RAPL and HCTZ was dependent on dendrimer concentration and pH of dendrimer solution. The solubility profile of both RAPL and HCTZ dendrimer complexes illustrated a non‐linear relationship with dendrimer concentration. At 0.8% (w/v) dendrimer concentration, solubility of RAPL was increased 4.91 folds with amine‐terminated while for HCTZ, solubility enhancement was highest (3.72 folds) with carboxy‐terminated. The complexes were characterized by Fourier transform infrared spectroscopy, nuclear magnetic resonance analysis and high performance liquid chromatography. In‐vitro drug dissolution performance of pure drugs, individual drug loaded dendrimer formulations and hybrid formulations was studied in USP dissolution medium (pH 7.0) and in simulated gastric fluid (pH 1.2). Dendrimer mediated formulations showed faster and complete dissolution compared to pure RAPL or HCTZ. Surprisingly, similar pattern of dissolution profile was established with hybrid formulations as compared to individual drug loaded dendrimers. The dendrimer‐based hybrid formulations were found to be stable at dark and refrigerated conditions up to 5 weeks. Conclusively, the proposed formulation strategy establishes a novel multitasking platform using dendrimer for simultaneous loading and delivery of multiple drugs for pharmaceutical applications. Graphical abstract Figure. No caption available.

Macroscopial, anatomical and physico-chemical studies on fruits of Coccinia indica Wight & Arn. (Cucurbitaceae)

Abstract Objective To rationalize the macroscopial, anatomical and physico-chemical studies on fruits of Coccinia indica Wight & Arn. (Cucurbitaceae). Methods The crude ethanolic extract of fruits of Coccinia indica Wight & Arn. (Cucurbitaceae) was using physico-chemical parameters, fluorescence analysis, and preliminary photochemical investigation (TLC, HPTLC, column chromatography). Results An attempt has been made to highlight this folk herbal medicine through present study which will assist in the identification of fresh as well as dried crude samples of fruits anatomically and physico chemically. TLC fingerprint profiling and fluorescence analysis of powdered fruits were also carried out and the salient qualitative and quantitative parameters are reported. Conclusions The present study will provide referential information for correct identification and help in checking adulteration in market samples used in the preparation of various herbal medicines. The present observation will also be helpful in macroscopial, anatomical and physico-chemical studies on fruits of Coccinia indica Wight & Arn. (Cucurbitaceae).

Pharmacognostic and phytochemical evaluation of Dolichos biflorus Linn.

Abstract Objective To study in detail the micromorphology and physicochemical analysis of the seeds of Dolichos biflorus Linn. (Family: Papileonaceae). Methods Macroscopy, microscopy, physicochemical analysis, preliminary phytochemical screening and other WHO recommended parameters for standardizations were performed. Results The seeds are roughly trapezoidal and flattish, with quite thin cotyledons. The hylum is small and linear and located in a small depression on the seeds lateral margin. The length of archeological specimens are usually 3.0–4.0 mm, width 2.0–2.6 mm and thickness 1.4–2.0 mm. Microscopic evaluation revealed the epidermis is single layered brown in colour, thin walled and shining cells because of mucilage in this layer. Endosperm forms bulk of the seed with thick walled polygonal parenchymatous cells. Outer portion of the seed contains alueron grains which are protein in nature. In the mid of the seeds, embryo can be seen which provides nutrition. Preliminary phytochemical screening showed the presence of steroids, tannins, proteins, aminoacids, flavonoids, terpenoids, mucilage, volatileoil, saponin and carbohydrates and absence of alkaloids, fixed oil. Conclusions The microscopic using histological identification, microscopic constants and other physico chemical examinations of the seeds of Dolichos biflorus Linn. can be used as a rapid, inexpensive botanical identification technique and is useful in standardization, hence it would be of immense value in authentication of seed.