scholarly journals Improvement of Pain Relief of Fentanyl Citrate Drug Encapsulated in Nanostructured Lipid Carrier: Drug Formulation, Parameter Optimization, in vitro and in vivo Studies

2020 ◽  
Vol Volume 14 ◽  
pp. 2033-2045
Author(s):  
Mohammad Amin Bahrami ◽  
Nafiseh Farhadian ◽  
Mohammad Karimi ◽  
Arash Forouzan ◽  
Kambiz Masoumi
2020 ◽  
Vol 13 ◽  
Author(s):  
Ankita Dadwal ◽  
Neeraj Mishra ◽  
Raj Kumar Narang

Background: Psoriasis is an autoimmune disease of the skin with lapsing episodes of hyperkeratosis, irritation, and inflammation. Numerous traditional and novel drug delivery systems have been used for better penetration through psoriatic barrier cells and also for retention in the skin. As there is no effective remedy for better penetration and retention is there because of the absence of an ideal carrier for effective and safe delivery of antipsoriatic drugs. Objectives: The main objective of this project is to develop Squalene integrated NLC based carbopol 940 gel to create a local drug depot in skin for improved efficacy against psoriasis. Methods: Homogenization method is used for the formulation of Nanostructured Lipid Carrier and were characterized on the basis of size, entrapment efficiency, polydispersity index (PDI), viscosity, spreadability, DSC, zeta potential, % in vitro release, in vitro skin permeation and retention studies, physical storage stability studies and in vivo studies can use other alternative models for induction of psoriasis by severe redness, swelling macroscopically and microvascular dilation edema lasting for 10 days. Further histopathology study was done to basses of changes in the skin. Conclusion: The optimized formulation of nanostructured lipid carrier-based gel has shown significant sustained release of clobetasol propionate. Further, this formulation has also shown retention in skin because of squalene as it is sebum derived lipid show affinity towards the sebaceous gland.


2018 ◽  
Vol Volume 13 ◽  
pp. 8355-8364 ◽  
Author(s):  
Kuo-Sheng Liu ◽  
Wei-Hsun Chen ◽  
Cheng-Hung Lee ◽  
Yong-Fong Su ◽  
Shih-Jung Liu

2020 ◽  
Vol 21 (3) ◽  
pp. 1093
Author(s):  
Jian-Ming Chen ◽  
Kuan-Chieh Liu ◽  
Wen-Ling Yeh ◽  
Jin-Chung Chen ◽  
Shih-Jung Liu

In this study, we explored the release characteristics of analgesics, namely levobupivacaine, lidocaine, and acemetacin, from electrosprayed poly(D,L-lactide-co-glycolide) (PLGA) microparticles. The drug-loaded particles were prepared using electrospraying techniques and evaluated for their morphology, drug release kinetics, and pain relief activity. The morphology of the produced microparticles elucidated by scanning electron microscopy revealed that the optimal parameters for electrospraying were 9 kV, 1 mL/h, and 10 cm for voltage, flow rate, and travel distance, respectively. Fourier-transform infrared spectrometry indicated that the analgesics had been successfully incorporated into the PLGA microparticles. The analgesic-loaded microparticles possessed low toxicity against human fibroblasts and were able to sustainably elute levobupivacaine, lidocaine, and acemetacin in vitro. Furthermore, electrosprayed microparticles were found to release high levels of lidocaine and acemetacin (well over the minimum therapeutic concentrations) and levobupivacaine at the fracture site of rats for more than 28 days and 12 days, respectively. Analgesic-loaded microparticles demonstrated their effectiveness and sustained performance for pain relief in fracture injuries.


2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Yasmeen Taj ◽  
Roopa S. Pai ◽  
V. Kusum Devi ◽  
Gurinder Singh

The main aim of the present study was to evaluate the potential of orally disintegrating pellets (ODPs) as an approach for taste masking of bitter drugs, namely, Ambroxol hydrochloride (A-HCl) and Cetirizine dihydrochloride (C-DHCl). Pellets were prepared by extrusion/spheronization with Eudragit EPO, kyron T-134, Kyron T-314, mannitol, sorbitol, MCC (Avicel PH-101), sucralose, chocolate flavor, and 5% xanthum gum. The prepared pellets were characterized for percentage yield, drug content, particle size, in vitro drug release, and in vivo evaluation on humans for taste, mouth feel, and in vivo disintegration time. The results revealed that the average size of pellets was influenced greatly by the percentage of binder and extrusion speed. The optimized ODPs disintegrated in less than 20 s and showed more than 98% of drugs in ODPs dissolved within 15 min. Taste perception study was carried out on human volunteers to evaluate the taste masking ability of ODPs for taste, mouth feel, and in vivo disintegration time. Crystalline state evaluation of drugs in the optimized ODPs was conducted for X-ray powder diffraction. In conclusion, the study confirmed that ODPs can be utilized as an alternative approach for effective taste masking and rapid disintegration in the oral cavity.


2001 ◽  
Vol 5 (8) ◽  
pp. 645-651
Author(s):  
M. Peeva ◽  
M. Shopova ◽  
U. Michelsen ◽  
D. Wöhrle ◽  
G. Petrov ◽  
...  
Keyword(s):  

2005 ◽  
Vol 25 (1_suppl) ◽  
pp. S198-S198
Author(s):  
Joseph R Meno ◽  
Thien-son K Nguyen ◽  
Elise M Jensen ◽  
G Alexander West ◽  
Leonid Groysman ◽  
...  

1994 ◽  
Vol 72 (06) ◽  
pp. 942-946 ◽  
Author(s):  
Raffaele Landolfi ◽  
Erica De Candia ◽  
Bianca Rocca ◽  
Giovanni Ciabattoni ◽  
Armando Antinori ◽  
...  

SummarySeveral “in vitro” and “in vivo” studies indicate that heparin administration may affect platelet function. In this study we investigated the effects of prophylactic heparin on thromboxane (Tx)A2 biosynthesis “in vivo”, as assessed by the urinary excretion of major enzymatic metabolites 11-dehydro-TxB2 and 2,3-dinor-TxB2. Twenty-four patients who were candidates for cholecystectomy because of uncomplicated lithiasis were randomly assigned to receive placebo, unfractionated heparin, low molecular weight heparin or unfractionaed heparin plus 100 mg aspirin. Measurements of daily excretion of Tx metabolites were performed before and during the treatment. In the groups assigned to placebo and to low molecular weight heparin there was no statistically significant modification of Tx metabolite excretion while patients receiving unfractionated heparin had a significant increase of both metabolites (11-dehydro-TxB2: 3844 ± 1388 vs 2092 ±777, p <0.05; 2,3-dinor-TxB2: 2737 ± 808 vs 1535 ± 771 pg/mg creatinine, p <0.05). In patients randomized to receive low-dose aspirin plus unfractionated heparin the excretion of the two metabolites was largely suppressed thus suggesting that platelets are the primary source of enhanced thromboxane biosynthesis associated with heparin administration. These data indicate that unfractionated heparin causes platelet activation “in vivo” and suggest that the use of low molecular weight heparin may avoid this complication.


Sign in / Sign up

Export Citation Format

Share Document