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Objective: The objective of the present study was to compare the release effect of Luliconazole from different polymeric (Hydrophilic and Hydrophobic) microsponges prepared using varying concentrations. The best microsponge was selected and incorporated into different gel (Natural and synthetic) and drug release is determined and compared with marketed formulation. Methods: Polymers such as EC, HPMC, Eudragit RSPO and PVA as emulsifier, and solvent DCM is used as solvent. Microsponge were prepared by using the quasi emulsion solvent diffusion technique. FTIR was studied to estimate the incompatibility. Microsponges were evaluated for SEM, particle size, drug content, and In vitro diffusion studies. Optimized microsponge incorporated gel was prepared by using different gel (flax seed gel and Aerosil gel) were evaluated for pH, spreadability, extrudability, drug content and in vitro diffusion studies. Results: Theresults obtainedshowed no physical-chemical incompatibility between the drug and the polymers. EC, HPMC and EC combination was found to be a suitable polymer compared to Eudragit RSPO and other combination in preparation of microsponge. From the evaluation of microsponge, the optimized F1 formulations was incorporated into different gel (flax seeds, aerosil) and compared with marketed formulation in which MG-I (flax seed gel) was considered as good topical anti-fungal microsponge gel based on there physical parameters and drug release kinetics. Conclusion: Microsponge and microsponge gel were successfully prepared for Luliconazole and their evaluation studies of each dosage form revealed that topically applied microsponge gel possess immense potential to control the release rate of medicament to improve the bioavailability as well as patient compliance.

Cubosomes are the nanoparticles of bicontinuous, lyotropic cubic phases, comprised of curved lipid bilayers organized into a three-dimensional honeycomb (cavernous) like structures separating two internal aqueous channels and large interfacial area. Cubic phases are optically isotropic, very viscous, and solid-like (crystalline) with cubic crystallographic symmetry. They can encapsulate hydrophilic, hydrophobic and amphiphilic drug substances, which are able to target and control the release of the bioactive agent. The cosmetic industry has made progress in the development of products to overcome skin as a barrier and deliver the actives through the skin effectively. Drug incorporated cubosomes shows some unique advantageous like, protection from chemical and physiological degradation, in vivo drug release in a controlled manner and improving the bioavailability of drug while reducing the side effect. Cubosomes are pharmacologically inactive, non-irritant, non-toxic, effective, and cosmetically acceptable. Topical drug delivery can deliver drugs selectively to the specific site; this avoids fluctuations of drug levels and improves patient compliance and suitable local and systemic therapeutic effects. Cubosomal topical drug formulation shows outstanding potential advantages for their controlled and sustained drug delivery. This review article mainly focuses on cosmetic and topical applications of cubosomes.

The transdermal drug delivery system is an alternative method of administration of drugs. Most of the drugs are delivered by conventional oral, topical, intravenous, and intramuscular methods and are is of limited efficiency. However, now the clinical use of transdermal delivery is limited because of stratum cornea of the skin act as an effective barrier that limits the permeation of drugs through the skin. To overcome this disadvantage, there are Recent developments in transdermal drug delivery, such as the usage of nanoparticles i.e., liposomes, niosomes, transferosomes, ethosomes, nanoemulsion, virosomes, phytosomes, dendrimers, proniosomes, microneedles, and separable microneedles. This nanoparticulate transdermal drug delivery exhibits great potential to ensure drug permeation through the skin. They are very tiny carriers to detect by the immune system and further, they can be delivering the drug to the targeted site and also have the ability to deliver both hydrophilic and hydrophobic drugs by reducing the complexity. Nanoparticles are made of different materials and they’re very different in structure and chemical properties are discussed in this review article.

Rapid dissolving oral film is the most advanced solid oral drug delivery system, that dissolve or disintegrate with in few seconds once placed in mouth without taking water or chewing. Drug directly reaches into systemic circulation therefore avoids first pass metabolism so bioavailability of medication may be improved. Now a days most of the pediatric, geriatric and dysphagia patients who find difficulty in swallowing, the rapid dissolving oral films often helps to overcome such type of complications. In terms of stability, handling, administration, and distribution, rapid dissolving oral films have grater advantages than tablet, capsules, or syrups. These compositions pharmacological activity is demonstrated by disintegration followed by dissolving. Hence disintegration has a major role for facilitating drug activity and thus gain popularity among other dosage forms. In this review, more importance is given on utilization of various super disintegrants comparing with other disintegrants. The different biological sources of super disintegrants (natural and synthetic), their properties, concentrations and modification to improves disintegration time are also high- lighted in this article.

Lipid dosage forms are the most preferred delivery system for hydrophobic drug molecules. Lipid dosage forms has many advantages of higher degree of biocompatibility and versatility and also lipid dosage form gained more importance in recent years because of their ability to improve the solubility and bioavailability of drugs with poor water solubility. Lipid formulation can be altered in various ways to provide wide range of product requirements as per the disease condition, route of administration, toxicity and efficacy. Lipid formulations are most reliable strategy for formulating pharmaceuticals, for topical, oral, pulmonary, or parenteral delivery. Due to their capability as therapeutic agents, ideally, these lipid-soluble drugs are incorporated into inert lipid carriers such as oil, surfactant dispersion, liposomes, emulsion etc. Emulsion is one of the known systems since many years. Pharmaceutical application of the emulsion is widely speeded after the microemulsion and nano emulsions appearance. Microemulsions are clear, stable and isotropic mixture of oil, surfactant and cosurfactant. Emulsions and nano emulsions are not thermodynamically stable, compared with microemulsions. The main objective of this review paper is to discuss about the effect of oil, surfactant and cosurfactant on the microemulsions.

Microsponge a drug delivery system, possesses the versatility to load a wide range of active ingredients due large surface area. it facilitates controlled release of active ingredients and reduces systemic exposure and adverse effect. microsponges are polymeric sponges that consist of interconnecting voids with a flexible structure with a porous surface. Microsponge delivery techniques provides extended product stability, enhanced safety, enhanced formulation flexibility, product efficacy and aesthetic appeal with reduced adverse effects. It is regarded as safe, due to less bacterial contamination as it doesn’t require preservatives in the formulation. Therefore it is used in various sterile formulations like ophthalmic, parenteral etc. This review provides an overview of microsponge technology with its methodology, mechanism, programmable release, characterization and recent data on marketed formulations, their applications, and the list of patents, evaluation and application of microsponges in various aspects. Microsponge are frequently used for topical application but recently used for oral also.

Pharmacogenomics combines traditional pharmaceutical sciences such as biochemistry with annotated knowledge of genetics, protein chemistry, and DNA polymorphisms. The difference of therapeutic efficacy of the same drug in different individual can be best explained by the study of genetic polymorphisms that underlie individual differences in drug response. The small change of the genome in one individual may make a drug inefficacious as oppose to the other patients. Such variability will bring the individualization of the therapy to obtain the best effects of the drug, as an example autologous dendrimer got a tremendous success in the cancer therapy of the individual. Markers of exposure can determine whether the desired target tissues of a subject have been exposed to a drug at physiological concentrations. Gene expression profiling is a tool that can be used to characterize chemically induced toxicity in cells and/or animal models, in order to provide plausible explanations for observed toxicity in preclinical testing. Pharmacogenomics holds the promise that drugs might one day in future be tailor-made for individuals and adapted to each person's own genetic makeup by the use of microarray technology to express the gene which in turn helps to develop receptor protein. The stability of the drug and its toxicity can be predicted prior to administration of the drug to the subject through the knowledge of computer assisted structural simulation and DNA reactivity technology respectively. This article provides some critical aspects of drug developments, clinical trial design and ethical issues which are centered with pharmacogenomics.

The objective of present investigation was to prepare & evaluate the solid lipid nanoparticle (SLN) based gel using an antifungal agent Miconazole nitrate (MN). Compatibility of drug and excipients were confirmed by IR studies. The formulation was prepared by Micro emulsion and homogenization method using stearic acid and tween 80. All the Solid lipid nanoparticle formulations were subjected to particle size, drug entrapment efficiency, scanning electron microscopy and Differential Scanning Calorimetry. Formulation F2 resulted in least SLN particle size. The F3-SLN dispersion showed higher entrapment efficiency of 78.7%. Scanning Electron Microscopy of prepared SLN particles showed that prepared particles were spherical in shape and surface was rough. The Differential Scanning Calorimetry of the SLN particles showed conversion of drug from crystalline to amorphous state. The prepared SLN particles were dispersed in HPMC Carbopol gel. The resulting SLN loaded gels were evaluated for appearance, spreadability and in vitro drug release. The SLN loaded gels showed good appearance and spreadability. The invitro drug release of SLN gel was evaluated using Franz diffusion cell using dialysis membrane 70 with phosphate buffer pH 7.4 as a dissolution media. All the formulations showed drug release till 24hrs. It was concluded that Miconazole Nitrate loaded SLN gel formulation containing Carbopol 940 in combination with Hydroxy Propyl Methyl Cellulose was suitable for topical application since it showed prolonged drug release.

We report a comparative investigation of the characteristics of modified TiO2 nanorods grown on conducting indium tin oxide glass (ITO) substrates by two different hydrothermal methods: the direct method by which rutile TiO2 nanorods were grown directly on plain ITO substrates and the seed-mediated one using which a thin film of anatase TiO2 seed layer was laid down by spin coating and annealing prior to the growth of TiO2 nanorods on it. Microstructural analysis of the samples using X-ray diffraction confirmed their rutile nature. The average crystallite size estimated using Scherrer’s formula was found to fall in the range of 11–17 nm in both cases. Field emission scanning electron microscopy revealed the nanorod morphologies of a dandelion arrangement in the case of directly grown ones and a proper vertical orientation in the case of the seed-mediated method. UV–Vis spectroscopy analysis of both the samples exhibited redshifts with intense absorption of visible radiation, and the seed-mediated one was found to possess an increased bandgap. The transport nature of the samples was characterized by significant increase in both dark and photocurrents. The results show that the dark and photocurrent values of the directly grown TiO2 nanorods were greater than those of the seed-mediated ones by ~seven and five folds, respectively, and therefore, it could serve as efficient photoelectrodes in dye-sensitized solar cells.

Introduction The routine antenatal sonographic investigations of the umbilical cord are limited for assessment of number of umbilical vessels and doppler evaluation of umbilical blood flow. With the advancements of the sonographic techniques it is now possible to have more detailed evaluation of umbilical cord. There exist only few literatures on assessment of umbilical cord cross-sectional area during pregnancy to provide a baseline reference value. Aim To establish the reference intervals of cross-sectional area of the umbilical cord during gestation and to find the correlation of umbilical cord cross-sectional area with the foetal anthropometric measurements. Materials and methods This study was conducted among 214 normal pregnant women who underwent a routine antenatal sonogram during gestational age ranging from 24-39 weeks in the Department of Radiodiagnosis. The umbilical cord cross-sectional area was calculated at a plane immediately close to the umbilical cord insertion to the foetal abdomen. The following foetal parameters were studied: Biparietal Diameters (BPD), Head Circumference (HC), Abdominal Circumference (AC), Femur Length (FL), and Estimated Foetal weight (EFW). The relationship between foetal anthropometric measurements and umbilical cord cross sectional area was assessed using spearman rank correlation. The 5th, 10th, 50th, 90th and 95th percentiles of umbilical cord cross-sectional area were calculated for each gestational groups using polynomial regression analysis. Results A statistically significant correlation was observed between cross-sectional area of umbilical cord with both gestational age and foetal anthropometric parameters. The mean age of study population was 25.08±3.5 years and the mean gestational age was 34.42±2.5 weeks. We observed a strong correlation between head circumference and umbilical cord cross-sectional area. Conclusion The mean umbilical cord cross-section area increases steadily with gestational age for up to 34 weeks and then it declines. Umbilical cord cross-sectional area can be easily measured and hence it can be included in routine antenatal sonographic evaluations to predict the perinatal outcome. Careful monitoring of the pregnancy is needed in case of abnormal cross-sectional area measurements.

A basic concern of edentulous patients is retention of their dentures. This has led to considerable experimentation and research in efforts to perfect dentures that compensate for the loss of natural teeth. The use of multiple miniature suction cups made from a soft material lining the denture satisfies the requirements of retention and stability. A technique describing the fabrication of a maxillary and mandibular multicup dentures which are more beneficial than conventional complete dentures is discussed below with case report.

Pharmaceutical Chemistry Department, School of Advanced Sciences, Vellore Institute of Technology University, Vellore-632 014, Tamilnadu, India E-mail : jaya_saral@yahoo.com The comparative pharmacokinetic study of levodopa (l-dopa) nasal microspheres (test) and l-dopa carbidopa (c-dopa) nasal formulation (reference) was carried out on 120 healthy experimental rats in 20 groups. The concentration of l-dopa in brain was determined by LC/MS-MS. All pharmacokinetic parameters were calculated using a noncompartmental model. 90% bootstrap confidence interval (CI) of test/reference AUC and Cmax ratio were calculated to access bioavailability. The ratio and 90% CI for nasal l-dopa/nasal l-dopa+c-dopa formulation was 96.94 (60.05–133.83) for Cmax and 92.29 (66.54–118.04) for AUCt . Despite 90% CI limit not within the bioequivalence limit of 80% to 125% both formulation are equivalent at ratio test. The above statement is further proved by student t-test as probability of detecting difference between above formulations, at 95% CI was 0.547 which signifies there is no significant difference between two formulations. Therefore it can be concluded that bioadhesive nasal microspheres containing l-dopa alone can be used in treatment of Parkinson’s disease.

The protection against ethanol-induced lipid peroxidation is rendered by antioxidants such as vitamin E and glutathione (GSH) interacting with each other and also functioning independently. A study of the levels of GSH and activities of glutathione peroxidase (GP), glutathione reductase (GR) and glutathione transferase (GST) in the cerebral cortex (CC), cerebellum (CB) and brain stem (BS) of vitamin E-supplemented and -deficient rats subjected to ethanol administration for 30 days was carried out. Chronic ethanol administration to vitamin E-supplemented rats elevated GP, GR and GST activities in the three regions and GSH levels in the CB. Chronic ethanol administration to vitamin E-deficient rats elevated GR activity in the three regions and GP activity in the CC and CB, decreased GST activity in the CC and CB, but did not alter GSH levels compared with normal rats subjected to chronic ethanol administration. The results indicate that vitamin E helps to maintain GSH levels to combat increased peroxidation while its absence has a deleterious effect.

Drugs of abuse such as morphine or marijuana exert their effects through the activation of G-protein-coupled receptors (GPCRs), the opioid and cannabinoid receptors, respectively. Moreover, interactions between either of these receptors have been shown to be involved in the rewarding effects of drugs of abuse. Recent advances in the field, using a variety of approaches, have demonstrated that many GPCRs, including opioid, cannabinoid, and dopamine receptors, can form associations between different receptor subtypes or with other GPCRs to form heteromeric complexes. The formation of these complexes, in turn, leads to the modulation of the properties of individual protomers. The development of tools that can selectively disrupt GPCR heteromers as well as monoclonal antibodies that can selectively block signaling by specific heteromer pairs has indicated that heteromers involving opioid, cannabinoid, or dopamine receptors may play a role in various disease states. In this review, we describe evidence for opioid, cannabinoid, and dopamine receptor heteromerization and the potential role of GPCR heteromers in pathophysiological conditions.

Purpose: To evaluate the effect of formulation variables on the bioadhesion and release properties of bioadhesive cyproheptadine hydrochloride tablets. Methods: Screening of polymers - hydroxypropyl methylcellulose, (HPMC), sodium carboxy methyl cellulose (CMC), and Carbopol 974p and 934p - in solution form were carried out by shear stress and detachment force measurement,based on Taguchi model, in order to determine their bioadhesion properties. Central composite design (CCD) was applied to optimize the combined effects of the polymers on release rate constant (K), diffusion coefficient (n), regression coefficient (R 2 ) and detachment force of a sustained release tablet formulation of cyproheptadine hydrochloride containing also a prompt dose of the drug. Results: The shear stress of 3 % solution of HPMC was greater than that of an equivalent concentration of Carbopol 934P. The values of K, n, R 2 and detachment force for the optimized formulation (F0) were 0.269, 0.696, 0.964 and 0.066 Newton (N), respectively, and showed good correlation with the predicted values, thus confirming the practicability and validity of the model. Conclusion: Gastric retention time can be increased for cyproheptadine hydrochloride by formulating it as a bioadhesive tablet that enhances the retention of the dosage form in the stomach and hence gastric absorption of the drug. Keywords: Cyproheptadine hydrochloride, Bioadhesive core tablet, Detachment force, Taguchi design, Central composite design

Lymphatic filariasis (LF) is targeted for global elimination. Repeated annual single-dose mass treatment with antifilarials has been recommended as the principal strategy to achieve LF elimination. This requires an effective and sustainable strategy to deliver the drug diethylcarbamazine (DEC) to communities. In this study a new drug delivery strategy--community-directed treatment (comDT)--was developed and implemented and its effectiveness compared with that of the traditional health services-organized drug delivery in rural areas of Tamil Nadu India. Qualitative and quantitative data showed that the communities and health services were able to distribute the drug in almost all villages. The drug distribution rate and treatment compliance rate of comDT and health services treatment were statistically compared after adjusting them for clustering. Under the comDT 68% (n = 20 villages; range: 0-97%) of the population received DEC compared with 74% (n = 20 villages; range: 48-95%) with the health services treatment strategy (P > 0.05). However only about 53% (range: 0-91%) of comDT recipients and 59% (range: 32-79%) of those who received DEC from the health services consumed the drug (P > 0.05). Although statistically not significant the distribution and compliance rates were lower under the comDT strategy. Also the strategys operationalization appears to be difficult because of some social factors and the tradition of communities dependence on health services for treatment whereas health services-organized distribution was much less cumbersome and found to be more acceptable to people. However the distribution (74%) and compliance rates (59%) achieved by health services were also only moderate and may not be adequate to eliminate LF in a reasonable time frame. Health services manpower alone may not be sufficient to distribute the drug. The authors conclude that drug distribution by health services is the best option for India and participation of the community volunteers and village level government staffs in the program is necessary to effectively distribute the drug and attain the desirable levels of treatment compliance to eliminate LF. (authors)

This paper reports on DEC distribution and compliance with treatment in a large-scale annual single-dose mass treatment programme to eliminate lymphatic filariasis in the south Indian state of Tamil Nadu. 76.9% of households (82.5% in rural areas and 58.0% in urban areas) were aware of drug distribution for control of filariasis. DEC was given to 70% (= distribution rate) (range 0-92%) of the population and 53.5% (range 12-89%) complied with treatment. The distribution rate was more than 75% in 74% of the villages and compliance was in the range of 51-75% in 76% of the villages. About 5% of the treated population reported side-effects. Distribution and compliance were higher in rural than urban areas and similar between males and females. Qualitative data showed that some socio-economic factors, logistic and drug-related problems and people's poor knowledge and perceived benefits of treatment played a role in a proportion of the population not receiving or taking the drug. The Tamil Nadu programme showed that large-scale repeated annual DEC mass treatment is feasible and that existing health services are capable of delivering the drug to all communities. While even poor to moderate compliance rates can reduce the vector transmission of infection to some extent, improved drug distribution and compliance with treatment are necessary to consolidate the gains of earlier rounds of treatment and achieve the goal of filariasis elimination within a reasonable time frame.

Summary. Danazol (4 mg/day/animal) and oestradiol-17\g=b\(100 \g=m\g/day/animal) were administered subcutaneously for 22 and 15 days respectively. The testis and epididymis were histochemically analysed for steroid dehydrogenases, NADH\x=req-\ diaphorase, glucose 6-phosphate dehydrogenase activity and lipids. Both steroids significantly reduced the weights of the testis and other accessory reproductive organs. The activities of \g=D\5-3\g=b\-and 17\g=b\-HSDwere markedly reduced in the seminiferous epithelium and interstitial cells of the testis. Sudanophilic lipids accumulated in the seminiferous tubules and the interstitium. Oestradiol generally had a greater effect than did danazol, but both probably affect the testicular function by inhibiting steroidogenesis.