Posted by admin on Jun 30, 2020 in |
The aim of this work is to design and develop a controlled release drug delivery system of the anti-acne agent (dapsone), also used as a leprostatic agent. Dapsone is a strong anti-inflammatory agent that makes it a more powerful treatment in dermatological disorders; its treatment in acne requires long term steady-state concentration in plasma. Poor patient compliance and long term treatment by an oral route leading to dapsone resistance, which stimulates the development of depot preparation. Depot injection consists of a PLGA polymer containing matrix, which gives control release up to 1 month. Microspheres were formed by solvent extraction/evaporation technique. Various parameters, like a selection of solvents, selection of drug: polymer ratio, glycolide: lactide ratio, and evaporation temperature, were important and optimized based on the results. The entrapment efficiency of microspheres was found between 40% to 70%. The initial burst of the drug was controlled and found to be 9.8% within 24 h of release. The inactive ingredients used for formulation development were found to be compatible based on...
Read More
Posted by admin on Jun 30, 2020 in |
The main objective of the current study was to develop a highly sensitive LC-MS/MS (liquid chromatography-tandem mass spectrometry) technique for the quantification of trifluridine (TFD) in human plasma. Chromatography was processed on Phenomenex-RP-C18 (5 µm, 250 mm × 4.6 mm) column comprising acetonitrile, methanol and 5 mM ammonium formate (45:40:15, v/v) as a mobile phase, infused at a flow of 0.8 ml/min. TFD and internal standard ?-thymidine (TMD) were separated from 150 ml plasma utilizing Phenomenex cartridges. Quantification of the [M+H] +ion of analyte was done with MRM (multiple reaction monitoring) modes in LC-MS/MS utilizing electro-spray ionization. The parent and product ions transitions were monitored atm/z 297-181 and m/z2 41–42 for TFD and TMD respectively. The linearity was processed in the concentration range of 5.0–2000.0 ng/ml with regression coefficient (r2) = 0.999. Method intra and inter-batch precision findings were <3.33% and intra and inter-batch accuracy findings at three different concentrations were within 97.34% to 103.74%. Matrix effects were calculated by determining the %CV values for High and Low QC...
Read More
Posted by admin on Jun 30, 2020 in |
Kidney stones are aggregations of minerals such as calcium, oxalate, phosphates, uric acid, cysteine, etc. which can obstruct any part of the urinary system. This can turn fatal if left untreated as the major route of excretion is blocked causing the toxicity level to rise in the body which might lead to organ failure, coma and death. Limonia acidissima (wood apple) and Apple cider vinegar were found to contain phytoconstituents which are the bioactive components responsible for the anti-urolithiatic activity. Nucleation and aggregation of Calcium oxalate crystals was performed in presence of test samples were based on the percentage inhibition calculated, the mixture of samples gave the highest inhibition (37%) followed by wood apple (25%) and apple cider vinegar (9%). Calcium oxalate crystals were allowed to grow similarly where wood apple (113%) gave better inhibition when compared to apple cider vinegar (82%). The crystals obtained were microscopically monitored to correlate with obtained spectrophotometric results. Brushite crystals were grown synthetically by single gel diffusion and were exposed to the extracts....
Read More
Posted by admin on Jun 30, 2020 in |
The present study describes formulation optimization, in-vitro evaluation and ex-vivo assessment of indomethacin loaded binary ethosomal gel using central composite design. Two formulation factors, concentration of lipid and concentration of ethanol were optimized for their effects on vesicle size (Y1), zeta potential (Y2), polydispersity index (Y3), entrapment efficiency (Y4) and % cumulative drug release (Y5). The lipid concentration was found to significantly affect particle size, zeta potential and in-vitro drug release and ethanol concentration was found to significantly affect zeta potential while the interaction effects varied with each response. On identification of optimum desirability, an optimized formulation was prepared, characterized and loaded into transdermal gel. The optimized ethosomal formulation showed observed values for Y1, Y2, Y3, Y4 and Y5 of 185.5nm, -27mV, 0.237, 87.86% and 45.65% respectively. Ethosomal gels were formulated using carbopol and HPMC and were characterized for pH, spreadability, drug content, viscosity, and % CDR wherein the optimized formulation showed values of 6.85, 31.07 g.cm/sec, 99.87%, 52000cP, and 56.11% respectively. Ex-vivo permeation study for the optimized ethosomal...
Read More
Posted by admin on Jun 30, 2020 in |
The oral route of drug administration is the most common and preferred method of delivery due to convenience and ease of ingestion, but it is problematic if the drug is poorly soluble. Sufficient drug absorption, reproducible bioavailability and pharmacokinetic profile of orally administered drug substances are highly dependent on the solubility of that compound in an aqueous medium. Also, the therapeutic effectiveness of drugs depends upon bioavailability and, ultimately, upon the solubility of drug molecules. Solid dispersions have attracted considerable interest as an efficient means of improving the solubility and hence bioavailability of a range of hydrophobic drugs. These systems are one of the most promising approaches for solubility enhancement. They are referred to a group of solid products consisting of at least two different components, generally a hydrophilic matrix and a hydrophobic drug (1-4). The aim of the present study was to improve the solubility and dissolution rate of Lercanidipine Hydrochloride (L) by formulating a solid dispersion with Polyvinyl pyrollidone (PVP-K30) and Guar gum. Central composite design (CCD) was employed...
Read More
