Current Issue : October - December Volume : 2014 Issue Number : 4 Articles : 7 Articles
Nowadays, herbal drugs are gaining more attention due to lesser toxic effects and low cost. Due to the miraculous powers of herbal drugs they are picking more popularity. However, herbal drugs have many disadvantages like instability in acidic pH and liver metabolism causes a lower therapeutic effect. To overcome these limitation usages of novel drug dosage form plays a vital role. They overcome the limitations of product misidentification, standardization and many others. Novel systems increase the efficacy and transport of the drug at the site of action. Traditional systems of administering herbal drugs are older and may cause either insufficient drug concentration at the site of action or drug accumulation. So Novel approaches like microspheres, nanoparticles, niosomes, phytosomes, complexation and nanoemulsions are useful. Incorporating herbal drug in these dosage forms improves bioavailability and efficacy. An industry also faces problems associated with herbal drugs, but they are trying to overcome them by using improvised analytical and extraction techniques. Industries are aware that they will make more profit by the use of herbal medicines as the market value of herbal drugs is getting higher....
The aim of the present investigation was to develop and characterize naproxen sodium loaded microemulsion based gel (MEBG) for treatment of rheumatoid arthritis. Screening of components was based on the drug solubility, HLB value and biocompatibility. Pseudo-ternary phase diagrams were constructed at different surfactant to co-surfactant ratios to identify the microemulsion (ME) existing zone. MEs were formulated by water titration method, optimized and characterized. Optimized ME was then formulated into MEBG by adding carbopol 934P as a gelling agent and was characterized. Comparative in-vitro drug release of formulations was studied for 12 hr and data fitted to different release kinetic models. Three months stability study was conducted as per ICH guidelines. % transmittance, globule size, zeta potential and drug content of optimized ME containing oleic acid as oil, tween-80 as surfactant and isopropyl alcohol as co-surfactant were found to be 99.8±0.2%, 16.62±3.5 nm, -24.3±1.66 mV and 99.03±0.35% respectively. Drug permeation data fit well to higuchi equation plot (r2 = 0.930) indicating the diffusion rate limited drug permeation from developed formulation. Drug permeation mechanism was found as a super case-II transport (i.e., n value- 1.504). Developed ME was transparent, stable up to 2 months with nano particle size. Hence, developed microemulsion formulations of Naproxen sodium is considered to be safe for topical delivery to treat rheumatoid arthritis....
One of the most interesting and challenging activities faced by the pharmaceutical researchers was to develop novel drug delivery system for the attainment of optimal concentration at the intended site of action for the sufficient time period to elicit the therapeutic response. Advanced research on this concept led to the development of in-situ forming polymeric drug delivery systems. This system includes many advantages for sustained and controlled drug release in comparison with that of conventional drug delivery system and possesses ease of administration, reduced frequency of dosing, improved patient compliance and comfort. The production of these systems includes lower manufacturing costs and is economical. In-situ gels are in solution form upon instillation and it undergoes phase transition into visco-elastic gel form after contacting with biological fluids. The conversion from sol to gel depends upon certain factors like temperature modulation, pH change, presence of ions and ultra violet irradiation. Now a days in-situ gel are used as vehicles for the drug delivery for both systemic effects and local treatment. Various biodegradable polymers are used in the formulation of in-situ gels like pectin, xyloglucan, gellan gum, poly caprolactone, poly (DL lactic acid), carbomers, chitosan, etc. Mainly in-situ gels are administered by oral route, ocular route, nasal route, rectal and vaginal route, through injectable and intra-peritoneal route. The present review mainly includes different approaches of in-situ gel formations its applicability based on the routes of administration and some of the recent advancements of in-situ gels....
This study was aimed to statistically optimize coating of oxynutynin chloride tablet for pH dependant colon targeting delivery system. The core tablets were evaluated for pharmacopoeial and non pharmacopoeial test. Enzyme α-galactosidase concentration was defined by lactose degradation study. In presence of eudragit RL 100 release rate was significantly increased which proved hydrophilic characteristic of polymer improved water absorption and ultimately drug release. A 32 full factorial design was used for preparation of coating of tablet. The experimental design of coating of tablets comprised of two independent variables: amount of eudragit E 100 and acryl EZE, each at three different levels and the dependent variable were time required to release 50% and 85% of drug. The in-vitro drug release study of F1-F9 was carried out by change over media method (0.1 N HCl buffer, pH 1.2, phosphate buffer, pH 6.8 and enzymatic phosphate buffer, pH 6.8 with enzyme 2%) and F5 batch was optimized. Drug release mechanism was studied. Conclusively, pH dependant colon targeted oxynutynin chloride tablets were successfully optimized....
The purpose of this study was to enhance the dissolution pattern of the practically water insoluble antihypertensive drug, olmesartan medoxomil through its formulation into liquisolid tablets. A mathematical model was used to formulate many liquisolid powder systems using propylene glycol as a non-volatile water miscible liquid vehicle. The liquid loading factors of the vehicle were used to calculate the optimum quantities of carrier (Avicel PH 102) and coating materials (aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures. Different excipient (R) ratios were used (20, 30, 40 and 50). The liquisolid tablets were evaluated for weight variation, percent friability, hardness, content uniformity, disintegration time and in-vitro drug release profile. Differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FT-IR) were used for the assessment of the physicochemical properties of drug in the liquisolid tablets. The enhanced dissolution rate due to the increased wetting properties and the large available surface areas for dissolution were obtained in case of the liquisolid tablets. The selected optimal formulation (LS3) released 74.74% of its content during the first 5 min compared to 9.18% of the plain drug and 40.54% of directly compressible tablet. In conclusion, the dissolution rate of olmesartan medoxomil can be enhanced to a great extent by liquisolid technique....
The objective of this research was to improve the physicochemical properties of mosapride citrate (MSP) with an ultimate goal to increase its bioavailability. In order to achieve this goal, MSP-pharmacosomes were prepared by refluxing MSP and phospholipids at different temperatures, for different times and using different mosapride: phosphatidylcholine (PC) molar ratios. The yield % of prepared MSP-pharmacosomes was evaluated to determine the best preparation conditions. The best formula was characterized regarding N-octanol/water partition coefficient, N-octanol solubility; water solubility, FT-IR, differential scanning calorimetry (DSC), X-ray diffraction (XRD) morphology and particle size. Results revealed that reaction temperature 60°C for reaction time of 2 hrs using MSP: PC molar ratio 1:2 was the optimum conditions for MSP-pharmacosomes preparations. The prepared MSP-pharmacosmes partition coefficient was higher than MSP material. MSP-pharmacosomal dispersion in water had a small particle size in nano range. Accordingly, MSP-pharmacosomes could be a promising approach for improving physicochemical properties of mosapride citrate to increase its bioavailability....
Application of zotepine, an antipsychotic agent, was limited due to its low therapeutic index which in-turn due to its poor aqueous solubility and low oral bioavailability. Hence the aim of present study was to develop zotepine loaded nanoparticle (ZNP) to overcome the problems and also to improve its brain uptake. Zotepine loaded nanoparticles were prepared by solvent evaporation technique using biodegradable PLGA as carriers, PVA as surfactant and were evaluated. Zotepine loaded nanoparticles were optimized by evaluating particle size, zeta potential and % entrapment efficiency. TEM result confirmed the size distribution and morphology. Comparative brain uptake study was carried out through concentration achieved in brain and AUC for developed ZNPs and marketed formulation on male albino wistar rats by RP-HPLC method. Particle size, zeta potential and % E.E of optimized batch containing were found to be 259.13±3.42 nm, -23.3±3.02 mV and 70.41±2.71% respectively. Higher drug concentration at all-time points and also higher AUC for developed formulation suggesting effective CNS transport of drug. Findings of present investigation revealed that developed zotepine loaded nanoparticles through oral route could be a promising approach for brain targeting of zotepine....
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