11 research outputs found
Kinetic evaluation of L-Dopa loaded WGA-grafted nanoparticles
No full textDrug release is a critical parameter in the discipline of drug delivery for years. The determination of in vitro release kinetics of active substances from drug systems plays a critical role in predicting and managing of both efficacy and safety. Kinetics is more than a scientific goal; it is a fundamental quality parameter of all type of drugs. Kinetic models are developed to determine drug release from delivery systems which the released drug amount (Q) is plotted versus time; t or as a function of time Q=f (t). Kinetic models facilitate the understanding of release pattern in enabling to design an effective formulation. In this study wheat germ agglutinin (WGA) conjugated, L-Dopa loaded, poly lactic-co-glycolic acid (PLGA) nanoparticles were analyzed for determining the release pattern of L-Dopa. Higuchi, zero order, first order, Hixon Crowell and Korsmeyer-Peppas models were investigated. Hixson Crowell model was found to be the best fitted kinetic model in L-Dopa loaded nanoparticles (r2 =0.9828). [Med-Science 2020; 9(2.000): 385-8
Formulation and evaluation of diclofenac potassium fast-disintegrating tablets and their clinical application in migraine patients
No full textThe aim of this study was to prepare fast-disintegrating tablets (FDTs) of diclofenac potassium with sufficient integrity as well as a pleasant taste, using two different fillers and binders: Tablettose 70 (R) and Di-Pac (R). Tablets were made with direct compression method. Tablet properties such as porosity, hardness, and disintegration time were determined. Diclofenac potassium determinations were carried out using a validated spectrophotometric method for the analysis of drug. Furthermore, in vivo experiments were carried out to compare the analgesic effect and the time to relieve migraine headache between the commercial tablets and FDTs of diclofenac potassium against placebo. Results showed that FDTs of diclofenac potassium with durable structure and desirable taste can be prepared using both fillers and binders but tablets prepared with Di-Pac had a better taste so the tablet formulation containing Di-Pac was chosen for in vivo experiments. Placebo controlled in vivo trial demonstrated that 50 mg diclofenac potassium, administered as a single dose of FDTs or commercial tablets, was effective in relieving the pain and both of them were superior to placebo
Process and formulation variables of pregabalin microspheres prepared by w/o/o double emulsion solvent diffusion method and their clinical application by animal modeling studies
No full textPregabalin is an anticonvulsant drug used for neuropathic pain and as an adjunct therapy for partial seizures with or without secondary generalization in adults. In conventional therapy recommended dose for pregabalin is 75mg twice daily or 50mg three times a day, with maximum dosage of 600 mg/d. To achieve maximum therapeutic effect with a low risk of adverse effects and to reduce often drug dosing, modified release preparations; such as microspheres might be helpful. However, most of the microencapsulation techniques have been used for lipophilic drugs, since hydrophilic drugs like pregabalin, showed low-loading efficiency and rapid dissolution of compounds into the aqueous continous phase. The purpose of this study was to improve loading efficiency of a water-soluble drug and modulate release profiles, and to test the efficiency of the prepared microspheres with the help of animal modeling studies. Pregabalin is a water soluble drug, and it was encapsulated within anionic acrylic resin (Eudragit S 100) microspheres by water in oil in oil (w/o/o) double emulsion solvent diffusion method. Dichloromethane and corn oil were chosen primary and secondary oil phases, respectively. The presence of internal water phase was necessary to form stable emulsion droplets and it accelerated the hardening of microspheres. Tween 80 and Span 80 were used as surfactants to stabilize the water and corn oil phases, respectively. The optimum concentration of Tween 80 was 0.25% (v/v) and Span 80 was 0.02% (v/v). The volume of the continous phase was affected the size of the microspheres. As the volume of the continous phase increased, the size of microspheres decreased. All microsphere formulations were evaluated with the help of in vitro characterization parameters. Microsphere formulations (P1-P5) exhibited entrapment efficiency ranged between 57.00 +/- 0.72 and 69.70 +/- 0.49%; yield ranged between 80.95 +/- 1.21 and 93.05 +/- 1.42%; and mean particle size were between 136.09 +/- 2.57 and 279.09 +/- 1.97 mm. Pregabalin microspheres having better results among all formulations (Table 3) were chosen for further studies such as differential scanning calorimetry, Fourier transform infrared analysis and dissolution studies. In the last step, the best pregabalin microsphere formulation (P3) was chosen for in vivo animal studies. The pregabalin-loaded microspheres (P3) and conventional pregabalin capsules were applied orally in rats for three days, resulted in clinical improvement of cold allodynia, an indicator of peripheral neuropathy. This result when evaluated together with the serum pregabalin levels and in vitro release studies suggests that the pregabalin microspheres prepared with w/o/o double emulsion solvent diffusion method can be an alternative form for neuropathic pain therapy. Conclusively, a drug delivery system successfully developed that showed modified release up to 10 h and could be potentially useful to overcome the frequent dosing problems associated with pregabalin conventional dosage form
Enhancing Intracellular Uptake of Ivermectin through Liposomal Encapsulation
No full textIvermectin (IVM), an antiparasitic drug approved by the Food and Drug Administration (FDA), is widely used to treat several neglected tropical diseases, including onchocerciasis, helminthiases, and scabies. Additionally, IVM has shown potential as a potent inhibitor of certain RNA viruses, such as SARS-CoV-2. However, IVM is highly hydrophobic, essentially insoluble in water, which limits its bioavailability and therapeutic effectiveness. The use of liposomes as drug carriers offers several advantages, including enhanced solubility for lipophilic drugs, passive targeting of immune system cells, sustained release, and improved tissue penetration. To address the limitations of IVM, including its poor solubility and bioavailability, liposomal formulations were developed using a combination of soyphosphatidylcholine (SPC), dioleylphosphatidylcholine (DOPC), cholesterol (Ch), and diethylphosphate (DCP) in two distinct molar ratios (1.85:1:0.15 and 7:2:1) via the ethanol injection method. The physicochemical properties of the placebo and IVM-loaded liposomes were extensively characterized in our earlier study, including the particle size, polydispersity index, and zeta potential. The present work adds a deeper level of investigation into how to effect cellular uptake and cytotoxicity in vitro of both free IVM and IVM-loaded liposomes in Vero E6 cells. The half-maximal cytotoxic concentrations (CC₅₀) for free IVM and IVM-loaded liposomes were 10 μM and > 110 μM, respectively and the cellular uptake of IVM-loaded liposomes ranged from 13 to 60%, whereas free IVM showed a significantly lower uptake of only 2%. These results demonstrate that liposomal encapsulation effectively enhances IVM's cellular uptake while reducing its cytotoxicity, thus offering a promising strategy for improving the effectiveness of IVM
In vitro and in vivo evaluation of levodopa-loaded nanoparticles for nose to brain delivery
No full textParkinson's disease (PD) is a neurodegenerative disease which is characterized by the loss of dopaminergic neurons in the brain. Levodopa is the drug of choice in the treatment of PD but it exhibits low oral bioavailability (30%) and very low brain uptake due to its extensive metabolism by aromatic amino acid decarboxylase in the peripheral circulation. Moreover, levodopa has psychic, gastrointestinal, and cardiovascular side effects, and most importantly, short and frequent stimulation of dopamine receptors lead to undesirable conditions such as dyskinesia over time. The challenges are to increase the therapeutic efficiency, the bioavailability and decreasing the unfavourable side effects of levodopa. Biocompatible nano-sized drug carriers could address these challenges at molecular level. For this purpose, levodopa-loaded Poly (lactide-co-glycolide) acid nanoparticles were prepared by double emulsion-solvent evaporation method for nose to brain drug delivery. Parameters such as homogenization speed, and external and internal phase content were modified to reach the highest loading efficiency. F1-1 coded formulation showed prolonged release up to 9 h. Carbodiimide method was used for surface modification studies of nanoparticles. The efficacy of the selected nanoparticle formulation has been demonstrated by in vivo experiments in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine induced PD model in mice
The evaluation of sterile solutions of Ilwensisaponin A and C from Verbascum pterocalycinum var. mutense Hub.-Mor. on antiviral, antinociceptive and anti-inflammatory activities
No full textAntiviral, antinociceptive and anti-inflammatory activities of the 1% sterile solutions of Ilwensisaponin A and C isolated from the methanolic extract of the flowers of Verbascum pterocalycinum var. mutense Hub.-Mor. were investigated. Antiviral activities of sterile solutions were evaluated against Bovine Herpes Virus Type-1 (BHV-1) (Cooper strain). Both solutions showed cytotoxic effects. However, none of the sterile solutions showed antiviral activity with CPE values. Anti-inflammatory and antinociceptive response were obtained at doses of 100 mg/kg. The results of the evaluation of the anti-inflammatory activities induced by carrageenan showed that these sterile solutions possess active constituents and diminish cyclooxygenase activitiy. In addition, antinociceptive activities using p-benzoquinone-induced writhing model in mice of tested solutions were found to show notable activity in statistical analysis without inducing any apparent acute toxicity as well as gastric damage. To the best of our knowledge, this study is the first investigation of antiviral, anti-inflammatory and antinociceptive activities of sterile solutions of Ilwensisaponin A and C isolated from Verbascum pterocalycinum var. mutense Hub.-Mor. growing in Turkey. (C) 2019 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University
The evaluation of sterile solutions of Ilwensisaponin A and C from Verbascum pterocalycinum var. mutense Hub.-Mor. on antiviral, antinociceptive and anti-inflammatory activities
No full textAntiviral, antinociceptive and anti-inflammatory activities of the 1\%
sterile solutions of Ilwensisaponin A and C isolated from the methanolic
extract of the flowers of Verbascum pterocalycinum var. mutense
Hub.-Mor. were investigated. Antiviral activities of sterile solutions
were evaluated against Bovine Herpes Virus Type-1 (BHV-1) (Cooper
strain). Both solutions showed cytotoxic effects. However, none of the
sterile solutions showed antiviral activity with CPE values.
Anti-inflammatory and antinociceptive response were obtained at doses of
100 mg/kg. The results of the evaluation of the anti-inflammatory
activities induced by carrageenan showed that these sterile solutions
possess active constituents and diminish cyclooxygenase activitiy. In
addition, antinociceptive activities using p-benzoquinone-induced
writhing model in mice of tested solutions were found to show notable
activity in statistical analysis without inducing any apparent acute
toxicity as well as gastric damage. To the best of our knowledge, this
study is the first investigation of antiviral, anti-inflammatory and
antinociceptive activities of sterile solutions of Ilwensisaponin A and
C isolated from Verbascum pterocalycinum var. mutense Hub.-Mor. growing
in Turkey. (C) 2019 The Authors. Production and hosting by Elsevier B.V.
on behalf of King Saud University
