Preparation of tripterygium glycoside nanoparticles and therapeutic effect on arthritis rats / 中国药理学通报

Aim To prepare tripterygium glycoside nanoparticles and probe into their therapeutic effect on collagen-induced arthritis ( CIA) rats. Methods Tripterygium glycosides polyglycoside nanoparticles were prepared by thin film dispersion method and their quality was assessed. The CIA model was established and drug intervention performed. The body weight, toe swelling degree and arthritis index were measured. The pathological changes of the organs, knee and ankle synovium were observed. The serum levels of kidney function and inflammatory cytokine expression were detected in rats. Results The prepared tripterygium wil-fordii polyglycoside nanoparticles were round particles with uniform distribution and stable properties under electron microscope. Compared with the model group, the swelling of the left and right toes of medication group significantly decreased (P < 0. 01), and the ar-thritis index markedly decreased ( P < 0. 01). Among them, the efficacy of the TG-NPs group was better than that of the TG group. Compared with the normal group, the indexes of heart, spleen, kidney and testis all significantly decreased (P <0. 05, P<0.01). TG-NPs group had a significantly reduced pathological ankle-joint injury in knee cartilage and increased apoptotic synovial cells. Compared with the model group, the serum levels of ALT and BUN and CRE in TG-NPs group were significantly lower (P < 0. 05 ), and IL-1β, TNF-α and IL-6 levels decreased significantly (P <0. 05). Conclusions TG-NPs have good therapeutic effect on CIA through induction of synovial cell apoptosis and decrease of the expression of inflammatory cytokines. By intravenous injection of blood circula-tion, slow and controlled release of drugs can be achieved, the first pass effect caused by oral drug can be avoided, the viscera toxicity can be reduced, which provides an experimental basis for the development of new nanoagents for the treatment of rheumatoid arthritis.

Study of erythrocytes as a novel drug carrier for the delivery of artemether

Resealed erythrocytes have been explored in various dimensions of drug delivery, owing to their high biocompatibility and inability to initiate immune response. The present research was designed to evaluate the drug delivery potential of erythrocytes by loading a hydrophobic anti-malarial drug, Artemether. Three different loading techniques were applied to achieve maximum optimized drug loading. A HPLC method was validated for drug quantification in erythrocytes. The relatively high loading was achieved using hypotonic treatment was 31.39% as compared to other two methods. These, drug loaded erythrocytes were characterized for membrane integrity via ESR showing higher ESR values for drug loaded cells as compared to normal cells. Moreover, microscopic evaluation was done to observe morphological changes in erythrocytes after successful loading which showed swollen cells with slight rough surface as compared to smooth surface of normal cells. Drug release was studied for 8 h which showed more than 80% release within 3-7 h from erythrocytes treated with different hypotonic methods. Overall, the study revealed a potential application of erythrocytes in delivery of hydrophobic drugs using hypotonic treatment as compared to other methods.

A review on nanoparticles – preparation and evaluation parameters.

Nanotechnology defined as a tiny science. Design characterization, production and applications of structures, devices and systems by controlling shape and size at nanometer scale is refers to nanotechnology. Nanotechnology by which we can achieve better therapeutic action, better bioavailability and better patient compliance. Several nanoformulations are successfully used for brain delivery which includes nanoparticles system (polymeric/solid lipid), liposomes, dendrimer‟s, nanoemulsions, nanosuspension and ligand mediated nanosystems.Nanoparticles are defined as particulate dispersions or solid particles drug carrier that may or may not be biodegradable. Several techniques are used for preparation of nanoparticles like Solvent Evaporation, Double Emulsification method, Emulsions - Diffusion Method, Nanoprecipitation, Coacervation method, Salting Out Method, Dialysis and Supercritical fluid technology. Nanoparticles are subjected to several evaluation parameters such as yield of nanoparticles, Drug Content / Surface entrapment / Drug entrapment, Particle Size and Zeta Potential , Surface Morphology, Polydispersity index, In-vitro release Study, Kinetic Study, Stability of nanoparticles.

Research progress on local pharmacokinetics of novel drug delivery system of Chinese materia medica / 中草药

With rapid development of modern science and technology, much progress has been made in novel drug delivery system of Chinese materia medica (CMM), combined with new polymer materials and multidisciplinary knowledge. Compared with the traditional preparation, novel drug delivery system in drug distribution in vivo presented high selectivity. In addition, there was no clear correlation between drug concentration in blood and efficacy. Pharmacokinetic process in local target in effect should therefore be systematically investigated. In this article, the author reviewed the means and technology of local pharmacokinetic study on novel drug delivery system for CMM, as well as progress made, and further discussed the developmental issues and challenges.

Bioavailability enhancers of herbal origin：An overview

Recently, the use of herbal medicines has been increased all over the world due to their therapeutic effects and fewer adverse effects as compared to the modern medicines. However, many herbal drugs and herbal extracts despite of their impressive in-vitro findings demonstrates less or negligible in-vivo activity due to their poor lipid solubility or improper molecular size, resulting in poor absorption and hence poor bioavailability. Nowadays with the advancement in the technology, novel drug delivery systems open the door towards the development of enhancing bioavailability of herbal drug delivery systems. For last one decade many novel carriers such as liposomes, microspheres, nanoparticles, transferosomes, ethosomes, lipid based systems etc. have been reported for successful modified delivery of various herbal drugs. Many herbal compounds including quercetin, genistein, naringin, sinomenine, piperine, glycyrrhizin and nitrile glycoside have demonstrated capability to enhance the bioavailability. The objective of this review is to summarize various available novel drug delivery technologies which have been developed for delivery of drugs (herbal), and to achieve better therapeutic response. An attempt has also been made to compile a profile on bioavailability enhancers of herbal origin with the mechanism of action (wherever reported) and studies on improvement in drug bioavailability, exhibited particularly by natural compounds.

Bioavailability enhancers of herbal origin: an overview

Recently, the use of herbal medicines has been increased all over the world due to their therapeutic effects and fewer adverse effects as compared to the modern medicines. However, many herbal drugs and herbal extracts despite of their impressive in-vitro findings demonstrates less or negligible in-vivo activity due to their poor lipid solubility or improper molecular size, resulting in poor absorption and hence poor bioavailability. Nowadays with the advancement in the technology, novel drug delivery systems open the door towards the development of enhancing bioavailability of herbal drug delivery systems. For last one decade many novel carriers such as liposomes, microspheres, nanoparticles, transferosomes, ethosomes, lipid based systems etc. have been reported for successful modified delivery of various herbal drugs. Many herbal compounds including quercetin, genistein, naringin, sinomenine, piperine, glycyrrhizin and nitrile glycoside have demonstrated capability to enhance the bioavailability. The objective of this review is to summarize various available novel drug delivery technologies which have been developed for delivery of drugs (herbal), and to achieve better therapeutic response. An attempt has also been made to compile a profile on bioavailability enhancers of herbal origin with the mechanism of action (wherever reported) and studies on improvement in drug bioavailability, exhibited particularly by natural compounds.

Isolation and characterization of novel mucoadhesive biomaterial from Phoenix dactylifera.

Phoenix dactylifera belongs to the family Arecaceae. The current aim of our research work is to isolate bio-material from the fruit pulp of Phoenix dactylifera and evaluate its mucoadhesivity. The bio- material was isolated by simple economical process. The isolated biomaterial was subjected for determination of solubility, colour changing point, viscosity, surface tension, pH and chemical tests. The mucoadhesivity of the biomaterial was assessed by shear stress method and rotating cylinder method using Capra aegagrus labium and intestine as mucosal substrates. The results were compared with HPMC and sodium CMC. The research study revealed that the biomaterial from Phoenix dactylifera exhibits promising inbuilt mucoadhesivity. So it can serve as a powerful natural mucoadhesant and may be used to develop mucoadhesive transmucosal drug delivery systems.

Isolation and characterization of novel mucoadhesive biomaterial from Phoenix dactylifera.

Phoenix dactylifera belongs to the family Arecaceae. The current aim of our research work is to isolate bio-material from the fruit pulp of Phoenix dactylifera and evaluate its mucoadhesivity. The bio- material was isolated by simple economical process. The isolated biomaterial was subjected for determination of solubility, colour changing point, viscosity, surface tension, pH and chemical tests. The mucoadhesivity of the biomaterial was assessed by shear stress method and rotating cylinder method using Capra aegagrus labium and intestine as mucosal substrates. The results were compared with HPMC and sodium CMC. The research study revealed that the biomaterial from Phoenix dactylifera exhibits promising inbuilt mucoadhesivity. So it can serve as a powerful natural mucoadhesant and may be used to develop mucoadhesive transmucosal drug delivery systems.

Novel Mucoadhesive Polymers –A Review.

The current article focuses on polymers used in mucosal delivery of therapeutic agents. The mucoadhesive drug delivery system is a popular novel drug delivery method because mucous membranes are relatively permeable, allowing for the rapid uptake of a drug into the systemic circulation and avoiding the first pass metabolism. Mucoadhesive polymers have been utilized in many different dosage forms in efforts to achieve systemic delivery of drugs through the different mucosa. These dosage forms include tablets, patches, tapes, films, semisolids and powders. The objective of this review is to study about novel mucoadhesive polymers and to design improved drug delivery systems.

Mouth dissolving tablets- a novel drug delivery system.

The past decade has thrown open the doors for continuous technological advancements in the pharmaceutical sector. Mouth Dissolving Tablets are one of the fruitful results of these technological advancements. MD tablets play a major role in improving the patient’s compliance. They rapidly disintegrate in the saliva hence obviating the need of the water. With the increasing incidences of non-compliance among the patients, Mouth dissolving tablets are the perfect answer to all these problems. A variety of drugs can be administered in the form of MD tablets as they give the advantage of the liquid medication in the solid preparation. These novel types of dosage forms have found acceptance among the geriatric, pediatric and dysphagic patients.

Topical treatment in vitiligo and the potential uses of new drug delivery systems.

Vitiligo is a psychologically devastating condition. Topical therapy is employed as first-line treatment in localized vitiligo. Currently, several topical agents are available in many forms viz. methoxsalen (solution and cream), trioxsalen (solution), corticosteroids (gel, cream, ointment and solution) and calcineurin inhibitors (ointment and cream). Although topical therapy has an important position in vitiligo treatment, side-effects or poor efficacy affect their utility and patient compliance. Novel drug delivery strategies can play a pivotal role in improving the topical delivery of various drugs by enhancing their epidermal localization with a concomitant reduction in their side-effects and improving their effectiveness. The current review emphasizes the potential of various phospholipid based carriers viz. liposomes, transferosomes, ethosomes, lipid emulsions, solid lipid nanoparticles and organogels in optimizing and enhancing the topical delivery of anti-vitiligo agents, whilst reducing the side effects of drugs commonly used in its topical treatment.