Formulation and evaluation of self-nanoemulsifying drug delivery system of brigatinib: Improvement of solubility, in vitro release, ex-vivo permeation and anticancer activity

Author(s):  
Mohammad Javed Ansari ◽  
Mohammed Alnakhli ◽  
Turki Al-Otaibi ◽  
Osaid Al Meanazel ◽  
Md Khalid Anwer ◽  
...  
2009 ◽  
Vol 25 (2) ◽  
pp. 161-177 ◽  
Author(s):  
Bhavesh D. Kevadiya ◽  
Ghanshyam V. Joshi ◽  
Hasmukh A. Patel ◽  
Pravin G. Ingole ◽  
Haresh M. Mody ◽  
...  

Nanomaterials ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 2920
Author(s):  
Ameeduzzafar Zafar ◽  
Syed Sarim Imam ◽  
Nabil K. Alruwaili ◽  
Omar Awad Alsaidan ◽  
Mohammed H. Elkomy ◽  
...  

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.


2021 ◽  
Vol 14 ◽  
Author(s):  
Sarbjot Kaur ◽  
Ujjwal Nautiyal ◽  
Pooja A. Chawla ◽  
Viney Chawla

Background: Background: Olanzapine belongs to a new class of dual spectrum antipsychotic agents. It is known to show promise in managing both the positive and negative symptoms of schizophrenia. Drug delivery systems based on nanostructured lipid carriers (NLC) are expected to provide rapid nose-to-brain transport of this drug and improved distribution into and within the brain. Objective: The present study deals with the preparation and evaluation of olanzapine loaded NLC via the intranasal route for schizophrenia. Methods: Olanzapine-NLC were formulated through the solvent injection method using isopropyl alcohol as the solvent, stearic acid as solid lipid, and oleic acid as liquid lipid, chitosan as a coating agent, and Poloxamer 407 as a surfactant. NLC were characterized for particle size, polydispersity index, entrapment efficiency, pH, viscosity, X-ray diffraction studies, in-vitro mucoadhesion study, in- vitro release and ex-vivo permeation studies. The shape and surface morphology of the prepared NLC was determined through transmission electron microscopy. To detect the interaction of the drug with carriers, compatibility studies were also carried out. Results: Average size and polydispersity index of developed formulation S6 was 227.0±6.3 nm and 0.460 respectively. The encapsulation efficiency of formulation S6 was found to be 87.25 %. The pH, viscosity, in-vitro mucoadhesion study, and in- vitro release of optimized olanzapine loaded NLC were recorded as 5.7 ± 0.05, 78 centipoise, 15±2 min, and 91.96 % respectively. In ex-vivo permeation studies, the percent drug permeated after 210 min was found to be 84.03%. Conclusion: These results reveal potential application of novel olanzapine-NLC in intranasal drug delivery system for treatment of schizophrenia.


2016 ◽  
Vol 105 (11) ◽  
pp. 3387-3398 ◽  
Author(s):  
Emelie Ahnfelt ◽  
Erik Sjögren ◽  
Per Hansson ◽  
Hans Lennernäs

1998 ◽  
Vol 550 ◽  
Author(s):  
E. J. Ginsburg ◽  
T. D. Stultz ◽  
D. A. Stephens ◽  
D. Robinson ◽  
Y. Tian ◽  
...  

AbstractThe dissolution of a drug delivery system consisting of gentamicin sulfate in a hydrophobic polyanhydride matrix has been examined. The in vitro release of gentamicin is a function of the composition of the dissolution medium, with slower release in pH 7.4 buffer than in unbuffered water. This is consistent with an anion exchange taking place under conditions in which carboxylate polymer chain-ends form a poorly soluble salt with gentamicin, and sulfate is released into solution. Results of additional experiments probing this model are digeussed.


2020 ◽  
Vol 15 (7) ◽  
pp. 425-429 ◽  
Author(s):  
Yuqiong Shi ◽  
Beibei Qiu ◽  
Xiangrong Wu ◽  
Yuxuan Wang ◽  
Jinhua Zhu ◽  
...  

2020 ◽  
Vol 52 (11) ◽  
pp. 1265-1274
Author(s):  
Zhijuan Zhao ◽  
Xiaodong Cui ◽  
Xiaoli Ma ◽  
Zhuanhua Wang

Abstract The self-nanoemulsifying drug delivery system has shown many advantages in drug delivery. In this study, a self-nanoemulsifying drug delivery system of buckwheat flavonoids was prepared for enhancing its antioxidant activity and oral bioavailability. A nanoemulsion of buckwheat flavonoids was developed and characterized, and its antioxidant, in vitro release, and in vivo bioavailability were determined. The nanoemulsion was optimized by the central composite design response surface experiment, and its particle size, polymer dispersity index (PDI), zeta potential, morphology, encapsulation efficiency, and stability were evaluated. The antioxidant activity was tested by measuring its 2,2-diphenyl-1-picrylhydrazyl scavenging activity, hydroxyl radical scavenging activity, and superoxide anion scavenging ability. In vitro release of buckwheat flavonoids nanoemulsion showed a higher cumulative release than the suspension, and the release fitting model followed the Ritger–Peppas and Weibull models. The effective concentration of the nanoemulsion was evaluated in vivo using a Wistar rat model, and the area under the plasma concentration-time curve of the buckwheat flavonoids nanoemulsion was 2.2-fold higher than that of the buckwheat flavonoid suspension. The Cmax of the nanoemulsion was 2.6-fold greater than that of the suspension. These results indicate that the nanoemulsion is a promising oral drug delivery system that can improve the oral bioavailability to satisfy the clinical requirements.


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