In vitro investigation on the impact of the surface-active excipients Cremophor EL, Tween 80 and Solutol HS 15 on the metabolism of midazolam

2004 ◽  
Vol 25 (1) ◽  
pp. 37-49 ◽  
Author(s):  
Roberto C. Bravo González ◽  
Jörg Huwyler ◽  
Franziska Boess ◽  
Isabelle Walter ◽  
Beate Bittner
Keyword(s):  
Tween 80 ◽  
Cremophor El ◽  
In Vitro Investigation ◽  
Surface Active ◽  
Solutol Hs 15 ◽  
The Impact

In vitro investigation on the impact of Solutol HS 15 on the uptake of colchicine into rat hepatocytes

2004 ◽  
Vol 279 (1-2) ◽  
pp. 27-31 ◽  
Author(s):  
Roberto Carlos Bravo González ◽  
Franziska Boess ◽  
Evelyne Durr ◽  
Nathalie Schaub ◽  
Beate Bittner
Keyword(s):  
Rat Hepatocytes ◽  
In Vitro Investigation ◽  
Solutol Hs 15 ◽  
The Impact

Design, Optimization and Characterization of Nanostructured Lipid Carriers of Raloxifene Hydrochloride for Transdermal Delivery

2020 ◽  
Vol 10 (1) ◽  
pp. 57-67 ◽  
Author(s):  
Durga Puro ◽  
Rajani Athawale ◽  
Anjali Pandya
Keyword(s):  
Particle Size ◽  
Transdermal Delivery ◽  
Tween 80 ◽  
Nanostructured Lipid Carriers ◽  
Polydispersity Index ◽  
Tape Stripping ◽  
Cremophor El ◽  
Scanning Calorimetry ◽  
Raloxifene Hydrochloride

Introduction: Raloxifene Hydrochloride (RXL), a BCS class II drug, is used for the treatment of invasive breast cancer and osteoporosis in post menopausal women. Even though the drug is highly efficient, it shows poor bioavailability of 2% when administered orally. The aim of the study was to develop, statistically optimize, and characterize Raloxifene Hydrochloride loaded Nanostructured Lipid Carriers (NLC) for transdermal delivery to overcome the bioavailability issue. Methods: The RXL-NLC’s were developed using glyceryl behenate (Compritol® 888 ATO), glyceryl monostearate (GMS), and capric triglyceride (Miglyol® 810) as solid and liquid lipids, and Polysorbate 80 (Tween 80) and cremophor EL were used as surfactants and co-surfactant. A response surface methodology was applied for the optimization of NLC, using Box-Behnken experimental design. Amount of the drug, tween 80 and polyethoxylated castor oil (cremophor EL), each at three levels, were selected as independent variables, while particle size and polydispersity index were identified as dependent variables. The optimized batch was characterized for Particle size (79.8 nm±3), Polydispersity index (0.229±0.05), Zeta potential (-12.3±5) and Entrapment efficiency (79.14%±5). Surface morphology of the NLC’s were studied using Transmission Electron microscopy (TEM) and the shift in the endotherm of Differential scanning calorimetry confirmed the entrapment of the drug within NLC. In vitro drug release studies were performed using dialysis bag (12000-14000 Da) method. The optimized NLC dispersion was then incorporated into gel and characterized for gel uniformity, spreadability, pH, viscosity and drug content. Results: In vivo skin penetration study was carried out by tape stripping method, which showed increase in penetration when incorporated into nanogel as compared to plain drug gel. Conclusion: Based on the above result it can be concluded that transdermal delivery of NLC’s can be a superior alternative for orally low bioavailable drugs such as RXL which undergoes rapid first pass metabolism.

Hybrid Liquisolid technique: A novel approach to enhance the in-vitro performance of antidiabetic drugs

2021 ◽  
Vol 16 ◽  
Author(s):  
Saloni Dalwadi ◽  
Vaishali T. Thakkar ◽  
Hardik B. Rana
Keyword(s):  
Tween 80 ◽  
Fixed Dose ◽  
Coating Materials ◽  
Boswellia Serrata ◽  
Peg 400 ◽  
Kneading Method ◽  
The Impact ◽  
In Vitro Performance

Background: A combination of Glimepiride and Boswellia serrata extract reduces Neuropathic diabetic complications by reducing the peroxidase level and improving the antioxidant level. The hybrid Liquisolid method includes a combination of two methods, kneading and the Liquisolid method to enhance drug in-vitro performance. Objective: The objective of this study was to enhance the in-vitro performance of antidiabetics drugs. Method: Tablets of the fixed dose combination of Glimepiride and Boswellia serrata extract were formulated by kneading method followed by Liquisolid method. Screening of non-volatile solvents, carriers, and coating materials was performed. The design of the experiment was applied to optimize the formulation and validation was done to validate the obtained model from the design of the experiment. 3 level 2 factorial (32) Design was applied by using Design expert software 11. Various pre-compression parameters were performed to check the quality of the formulation. Results: Screening of excipients for kneading method, Glimepiride with PVP K 30 (5%), and Boswellia serrata extract with Poloxamer 188 (13%) give optimum drug release. For the Liquisolid method Propylene glycol: PEG 400: Tween 80 (1:2:4) ratio for Glimepiride and PEG 400: Tween 80 (1:3) ratio for Boswellia serrata extract were selected. Common carrier and coating material for both drug Syloid XDP 3150: Aeroperl 300 (3:1) ratio were selected, which improves the in-vitro performance of the drug. Conclusion: This study gives an overall understanding of the impact of excipients on the quality of formulation, a critical knowledge to the implementation of this kind of novel application of Liquisolid systems.

scholarly journals In vitro investigation on the impact of airway mucus on drug dissolution and absorption at the air-epithelium interface in the lungs

2019 ◽  
Vol 141 ◽  
pp. 210-220 ◽  
Author(s):  
Emanuela Cingolani ◽  
Safar Alqahtani ◽  
Robyn C Sadler ◽  
David Prime ◽  
Snjezana Stolnik ◽  
...  
Keyword(s):  
Drug Dissolution ◽  
In Vitro Investigation ◽  
Airway Mucus ◽  
The Impact

scholarly journals Исследование свойств нового фотосенсибилизатора β,β,β',β'-тетраметилтрибензотетраазахлорина

2014 ◽  
Vol 48 (2) ◽  
pp. 7-12
Author(s):  
Антон Павлович Ластовой ◽  
Анастасия Александровна Игнатова ◽  
Алексей Валерьевич Феофанов ◽  
Елена Алексеевна Мачинская ◽  
Вероника Игоревна Иванова-Радкевич
Keyword(s):  
Tween 80 ◽  
Cremophor El

Проведен сравнительный анализ солюбилизаторов Cremophor EL, Tween 80, Эмуксол 3 и Pluronic F-68 по способности обеспечивать доставку перспективного фотосенсибилизатора β,β,β',β'-тетраметилтрибензотетраазахлорина (H2TBTAC) в клетки аденокарциномы легкого человека А549 in vitro. Обнаружено, что степень мономерности H2TBTAC в растворах рассматриваемых солюбилизаторов коррелирует с количеством флуоресцирующего мономера, накапливающегося в клетках. Доказана существенно более высокая способность мономера H2TBTAC к фотоиндуцируемой генерации синглетного кислорода по сравнению с агрегатами. Установлено, что Cremophor EL обеспечивает наибольшую мономерность H2TBTAC в растворе и наилучшую стабильность композиции при хранении. Cremophor EL способствует улучшенному накоплению мономерного H2TBTAC в цитоплазме клеток А549 с выходом на насыщение через 2 ч инкубации и максимальным коэффициентом накопления H2TBTAC равным 0,7 ± 0,1. В опытах in vivo показано наличие терапевтически значимого противоопухолевого эффекта фотодинамической терапии с использованием H2TBTAC, солюбилизированного в 10 % Cremophor EL.

scholarly journals Targeted Nanostructured Lipid Carrier for Brain Delivery of Artemisinin: Design, Preparation, Characterization, Optimization and Cell Toxicity

2018 ◽  
Vol 21 (1s) ◽  
pp. 225s-241s ◽  
Author(s):  
Jaber Emami ◽  
Hessam Yousefian ◽  
Hojjat Sadeghi
Keyword(s):  
Cancer Cell Line ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
In Vitro Cytotoxicity ◽  
Release Time ◽  
Nanostructured Lipid Carrier ◽  
Brain Delivery ◽  
Solvent Evaporation Method ◽  
The Impact

In the present study, a transferrin-conjugated nanostructured lipid carrier (TF-NLCs) for brain delivery of artemisinin (ART) was developed. ART-loaded NLCs (ART-NLCs) were prepared using solvent evaporation method and the impact of various formulation or process variables on the responses were assessed using a Taguchi design. Optimized ART-NLC was then coupled with transferrin as targeting ligand and its in vitro cytotoxicity was investigated against U-87MG brain cancer cell line. As a result, the following values are suggested by the software to prepare the optimized formulation: 20 mg Compritol®, 0.25% Tween 80, 5 mg oleic acid, 2.5 mL dichloromethane and 4 min sonication. Mean particle size (PS), zeta potential (ZP), polydispersity index (PDI), entrapment efficiency (EE), mean release time (MRT) of adopted formulation were confirmed to be 145 ± 12.5 nm, 24.3 ± 1.5 mV, 0.513 ± 0.021, 82.3 ± 7.3 % and 24.0 ± 1.1 h, respectively. Following conjugation of optimized ART-NLCs with TF, PS and MRT were increased, while ZP, and EE were decreased significantly. TF-ART-NLCs showed higher cytotoxic activity compared to non-targeted NLCs and free drug. These results indicated that the TF-ART-NLCs could potentially be exploited as a delivery system for anticancer and antimalarial drug ART in brain tumors and malaria.

scholarly journals In vitro investigation of the impact of pulsatile blood flow on the vascular architecture of decellularized porcine kidneys

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Peter R. Corridon
Keyword(s):  
Blood Flow ◽  
Blood Perfusion ◽  
Pulsatile Blood Flow ◽  
Venous Outflow ◽  
Venous Flow ◽  
Vascular Architecture ◽  
Arterial Perfusion ◽  
In Vitro Investigation ◽  
The Impact

AbstractA method was established using a scaffold-bioreactor system to examine the impact pulsatile blood flow has on the decellularized porcine kidney vascular architecture and functionality. These scaffolds were subjected to continuous arterial perfusion of whole blood at normal physiological (650 ml/min and 500 ml/min) and pathophysiological (200 ml/min) rates to examine dynamic changes in venous outflow and micro-/macrovascular structure and patency. Scaffolds subjected to normal arterial perfusion rates observed drops in venous outflow over 24 h. These reductions rose from roughly 40% after 12 h to 60% after 24 h. There were no apparent signs of clotting at the renal artery, renal vein, and ureter. In comparison, venous flow rates decreased by 80% to 100% across the 24 h in acellular scaffolds hypoperfused at a rate of 200 ml/min. These kidneys also appeared intact on the surface after perfusion. However, they presented several arterial, venous, and ureteral clots. Fluoroscopic angiography confirmed substantial alterations to normal arterial branching patterns and patency, as well as parenchymal damage. Scanning electron microscopy revealed that pulsatile blood perfusion significantly disrupted glomerular microarchitecture. This study provides new insight into circumstances that limit scaffold viability and a simplified model to analyze conditions needed to prepare more durable scaffolds for long-term transplantation.

scholarly journals Impact of Horse Hoof Wall with Different Solid Surfaces

2020 ◽  
Vol 10 (23) ◽  
pp. 8743
Author(s):  
Jing Zhao ◽  
Dan B. Marghitu ◽  
John Schumacher ◽  
Wenzhong Wang
Keyword(s):  
Contact Force ◽  
Coefficient Of Friction ◽  
Coefficient Of Restitution ◽  
Solid Surfaces ◽  
Effective Coefficient ◽  
In Vitro Investigation ◽  
Equine Hoof ◽  
Impact Angles ◽  
The Impact

This study aimed to investigate the impact of a horse hoof wall on three solid surfaces: steel, concrete and asphalt. Impact experiments were conducted for different impact angles and different initial impact velocities. The effect of impact surfaces, impact angles and initial impact velocities on the coefficient of restitution and the effective coefficient of friction were tested using one-way ANOVA. Analytical and numerical modeling of the impact were developed. The impact interval was divided into two phases: compression and restitution. For compression, a contact force with a damping term was used. The restitution was characterized by an elastic contact force. The stiffness and damping coefficients of the contact force were estimated from the normal impacts. The simulated velocities after the oblique impacts were compared to the velocities in the in vitro investigation. The coefficient of restitution varied significantly on different surfaces. The effective coefficient of friction was lower on steel compared to concrete and asphalt. The model presented in this study can be applied to refine the impact simulation of the equine hoof during locomotion.

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