TRANSDERMAL DRUG DELIVERY PATCHES: A REVIEW

For thousands of years, human civilizations have applied substances to the skin as cosmetic and medicinal agents. However, it was not until the twentieth century that the skin came to be used as a drug delivery route. In fact, Merriam Webster dates the word “transdermal†to 1944 highlighting that it is a relatively recent concept in medical and pharmaceutical practice. Transdermal drugs are selfâ€contained, discrete dosage form. Drug delivery through the skin to achieve a systemic effect without producing any fluctuations in plasma concentration of the drug.  Topical administration of therapeutic agents offers many advantages over conventional oral and invasive methods of drug delivery.  And also provide controlled release of the drug for extended period of the time. This review article covers brief outline advantages, skin pathways for transdermal drug delivery systems (TDDS), various components of transdermal patch, and approaches for preparation of transdermal patches, evaluation of transdermal system, general clinical considerations in the use of tdds and limitation of tdds. Key words: Transdermal, Permeation pathways, Drug delivery, Matrix, ReservoirÂ

DESIGN AND IN VIVO EVALUATION OF METOPROLOL TARTRATE BILAYER FLOATING TABLETS IN HEALTHY HUMAN VOLUNTEERS

The aim of the present investigation was to prepare bilayer floating tablets of metoprolol tartrate using the combination of superdisintigrants, HPMC K grade polymers and natural polymers like xanthan gum and guar gum by direct compression method. Bilayer floating tablets were prepared using optimized immediate release layer and floating layer as sustained release layer. The physico-chemical characteristics of the prepared tablets were evaluated and found to be satisfactory. All the prepared batches showed in vitro buoyancy. It was observed that the tablets remained buoyant for more than 12 h.  Formulation F7 was selected as best formulation based on the in vitro characteristics and used in vivo radiographic studies by adding barium sulphate. These studies revealed that the tablets remained in the stomach for 210±5.4 min (n=3) in fasting human volunteers. Based on the in vivo performance in healthy subjects, the developed bilayer floating tablets showed superior bioavailability than the marketed tablets, the drug release was up to 12 h in controlled manner. The systemic availability of the best formulation was high after administration to obtain immediate action due to the immediate release layer, from sustained release layer the drug was released in controlled manner. It can be concluded that the best formulation F7 by choosing biphasic drug release pattern in a single dosage form could improve patient compliance and ensure better disease management

Antimicrobial effects of Indian medicinal plants against acne-inducing bacteria

Propionibacterium acnes and Staphylococcus epidermidis have been recognized as pus-forming bacteria triggering an inflammation in acne. The present study was conducted to evaluate antimicrobial activities of Indian medicinal plants against these etiologic agents of acne vulgaris. Ethanolic extracts of Hemidesmus indicus (roots), Eclipta alba (fruits), Coscinium fenestratum (stems), Curcubito pepo (seeds), Tephrosia purpurea (roots), Mentha piperita (leaves), Pongamia pinnata (seeds), Symplocos racemosa (barks), Euphorbia hirta (roots), Tinospora cordyfolia (roots), Thespesia populnea (roots), and Jasminum officinale (flowers) were tested for antimicrobial activities by disc diffusion and broth dilution methods. The results from the disc diffusion method showed that 07 medicinal plants could inhibit the growth of Propionibacterium acnes. Among those Hemidesmus indicus, Coscinium fenestratum, Tephrosia purpurea, Euphorbia hirta, Symplocos racemosa, Curcubito pepo and Eclipta alba had strong inhibitory effects. Based on a broth dilution method, the Coscinium fenestratum extract had the greatest antimicrobial effect. The MIC values were the same (0.049 mg/ml) for both bacterial species and the MBC values were 0.049 and 0.165 mg/ml against Propionibacterium acnes and Staphylococcus epidermidis, respectively. In bioautography assay, the Coscinium fenestratum extract produced strong inhibition zones against Propionibacterium acnes. Phytochemical screening of Coscinium fenestratum revealed the presence of alkaloid which could be responsible for activity. Taken together, our data indicated that Coscinium fenestratum had a strong inhibitory effect on Propionibacterium acnes and Staphylococcus epidermidis. . Keywords: Acne; Propionibacterium acnes; Staphylococcus epidermidis; Antimicrobial activity > Tropical Journal of Pharmaceutical Research Vol. 6 (2) 2007: pp. 717-72

STUDIES ON GROUNDWATER QUALITY IN ANANTAPUR DISTRICT

ABSTRACT: Ground water is the main principal source for drinking water and other activities in Andhra Pradesh. It is the basic duty of every individual to conserve water resources. The present study attempts to bring an acute awareness among the people about the quality of ground water by taking water samples from 33 specific locations in Anantapur district to characterize the physicochemical parameters of Ground water. To assess the quality of groundwater, each parameter was compared with the standard desirable limit of that parameter in drinking water as prescribed by different agencies. This paper is a new study on water quality parameters in analyzing Anantapur district drinking water

DESIGN AND IN VIVO EVALUATION OF METOPROLOL TARTRATE BILAYER FLOATING TABLETS IN HEALTHY HUMAN VOLUNTEERS

The aim of the present investigation was to prepare bilayer floating tablets of metoprolol tartrate using the combination of superdisintigrants, HPMC K grade polymers and natural polymers like xanthan gum and guar gum by direct compression method. Bilayer floating tablets were prepared using optimized immediate release layer and floating layer as sustained release layer. The physico-chemical characteristics of the prepared tablets were evaluated and found to be satisfactory. All the prepared batches showed in vitro buoyancy. It was observed that the tablets remained buoyant for more than 12 h.  Formulation F7 was selected as best formulation based on the in vitro characteristics and used in vivo radiographic studies by adding barium sulphate. These studies revealed that the tablets remained in the stomach for 210±5.4 min (n=3) in fasting human volunteers. Based on the in vivo performance in healthy subjects, the developed bilayer floating tablets showed superior bioavailability than the marketed tablets, the drug release was up to 12 h in controlled manner. The systemic availability of the best formulation was high after administration to obtain immediate action due to the immediate release layer, from sustained release layer the drug was released in controlled manner. It can be concluded that the best formulation F7 by choosing biphasic drug release pattern in a single dosage form could improve patient compliance and ensure better disease management

FORMULATION AND EVALUATION OF LEVOFLOXACIN-CHITOSAN / β- CYCLODEXTRIN NANOPARTICLES BY IONIC GELATION

Background: Levofloxacin is a broad spectrum anti-infective agent, which is rapidly and completely absorbed after oral administration. The half life of Levofloxacin is 6-8 h after conventional dosing. The objective of the present work was to develop Levofloxacin nanoparticles to retain the dosage form in the absorption site more than the half life of the drug, enhance the bioavailability of drugs, reduce dose frequency, toxicity and patient compliance. Methods: The compositions of different formulations of Levofloxacin nanoparticles by the ionic gelation method using biodegradable polymer chitosan and tripolyphosphate as cross linking agent. Result and Discussion: The particle size lies of the prepared nanoparticles between 199 and 369 nm and the drug content found between 51.13± 0.28 and 71.12 ± 0.14 %. The particle size of nanoparticles increased with increasing concentration of polymer matrix density and this may be due to the increased viscosity of the inner phase and decreased with increasing concentration of β-cyclodextrin. Scanning electron microscopy indicated that the prepared nanoparticles were discrete, uniform and spherical with a smooth surface. The in vitro release showed that the drug release from the prepared nanoparticles was characterized by an initial fast release and followed by a delayed release phase. During and at the end of the accelerated stability study, the tested formulation showed almost same drug content, in vitro drug release and no colour changes were observed from that observed at the opening of the study. Conclusion: Among all the formulations (GIA, GIB, GIC, GID, GIE and GIF), the formulations G1C, G1E and G1F followed the drug release in a controlled manner. The in vitro release profile showed that this is a potential drug delivery for Levofloxacin and has to confirm in the in vivo settings as a separate investigation in future. Key words: Controlled drug delivery, In vitro drug release, Nanoparticle, Particle size, Stability studies, Surface morpholog

ANTIMICROBIAL, WOUND HEALING AND ANTIOXIDANT ACTIVITIES OF ANTHOCEPHALUS CADAMBA

Anthocephalus cadamba (Roxb.) Miq. Syn A. chinensis (Lamk) A. Rich (Rubiaceae) is ethnomedicinally widely used in the form of paste by tribe in western Ghats for treating skin diseases. In this context, antimicrobial potential of A. cadamba against a wide range of microorganisms was studied. To validate the ethnotherapeutic claims of the plant in skin diseases, wound healing activity was studied, besides antioxidant activity to understand the mechanism of wound healing. The alchoholic and aqueous extract of this plant showed significant antibacterial and antifungal activity against almost all the organisms: Micrococcus luteus, Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, and four fungi Candida albicans, Trichophyton rubrum—dermatophyte fungi, Aspergillus niger, Aspergillus flavus and Aspergillus nidulans—systemic fungi, with especially good activity against the dermatophyte (Trichophyton rubrum) and some infectious bacteria (Escherichia coli, Proteus mirabilis and Staphylococcus aureus) with an MIC of 2.5 µg/disc. The results show that A. cadamba extract has potent wound healing capacity as shown from the wound contraction and increased tensile strength. The results also indicated that A. cadamba extract possesses potent antioxidant activity by inhibiting lipid peroxidation and increase in the superoxide dismutase (SOD) and catalase activity

Synthesis of 4<i>H</i>-imidazo[2,1-<i>c</i>][1,4]benzo­xazin-4-yl acetic acids and esters as possible COX-2 inhibitors

792-795A series of 4H-imidazo[2,1-c][1,4]benzoxazin-4-yl acetic acids and esters (7 and 8) have been synthesized from methyl -(3,4-dihydro-3-oxo-2H-1,4-benzoxazin-2-yl)acetates 5 and their COX-2 inhibition activities are evaluated

HEPATOPROTECTIVE ACTIVITY OF HYDRO-ALCOHOLIC EXTRACT OF WHOLE PLANT OF SOLANUM DULCAMARA L. AND NEPHROLEPIS CORDIFOLIA (L) C. PRESL AGAINST PARACETAMOL INDUCE HEPATOTOXICITY IN ALBINO RATS

 Objective: To investigate the effect of hepatoprotective activity of hydro-alcoholic extract of Solanum dulcamara L. and Nephrolepis cordifolia (L)C. Presl against paracetamol induced hepatotoxicity in rats.Methods: Albino rats of either sex were divided into nine groups and treated for 7 days. Group I and II served as normal and toxic control, Group IIIwere treated with Silymarin (100 mg/kg), and Group IV to IX were treated with 200, 400 and 600 mg/kg hydro-alcoholic (70%v/v) extract ofS. dulcamara (HASD) and hydro-alcoholic (70%v/v) extract of N. cordifolia (HANC) respectively. The biochemical markers like serum glutamicpyruvictransaminase (SGPT), serum glutamic oxaloacetic transaminase (SGOT), alkaline phosphatase (ALP), bilirubin (total and direct), total protein,triglycerides (TG), total cholesterol (TC), high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C), very low-densitylipoprotein cholesterol (VLDL-C). The in vivo antioxidant activity was determined by estimating the tissue levels of glutathione (GSH), superoxidedismutase (SOD), catalase (CAT) and lipid peroxidation (LPO). Histopathology of liver was also carried out.Results: The HASD and HANC (200, 400 and 600 mg/kg) produced significant effect by decreasing the activity or level of SGOT, SGPT, ALP, billirubinand total protein, where decrease in total protein level in liver, TG, TC, LDL-C and VLDL-C levels and increase in the HDL-C. And decrease tissue LPO,while it significantly increased the levels of tissue GSH, SOD and CAT in a dose-dependent manner.Conclusion: From the present study it can be concluded that hydro-alcoholic extract of S. dulcamara L. and N. cordifolia (L) C. Presl whole plantpossesses hepatoprotective activity against paracetamol induced hepatotoxicity.Keywords: Hepatoprotective, In-vivo antioxidant activity, Paracetamol, Solanum dulcamara L. and Nephrolepis cordifolia (L) C. Presl, Silymarin