Comparative biodistribution and safety profiling of olmesartan medoxomil oil-in-water oral nanoemulsion

Gorain, Bapi; Choudhury, Hira; Tekade, Rakesh K.; Karan, Saumen; Jaisankar, Parasuraman; Pal, Tapan Kumar

doi:10.1016/j.yrtph.2016.10.020

Cited by 67 publications

(10 citation statements)

References 24 publications

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“…The collected animals were housed in polypropylene cages with 12-h light/12-h dark cycle at 25 ± 2°C and humidity of 50 ± 5 for acclimatization in standard environmental conditions. During the process of acclimatization for 10 days, the animals were provided with standard industrialized pellet foods and filtered water ad libitum (40). The protocol for the animal studies were conducted in accordance with the ethical rules of the ethics committee at the Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia, which had approved our experiments with application no.…”

Section: In Vivo Studymentioning

confidence: 99%

RETRACTED ARTICLE: ArticleNoteOptimization of Thymoquinone-Loaded Coconut Oil Nanostructured Lipid Carriers for the Management of Ethanol-Induced Ulcer

et al. 2020

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In the global incidence of peptic ulcer, with the associated rates of hospitalizations and mortality are increasing, in the United States, peptic ulcer disease affects approximately 4.6 million people annually, with an estimated 10% of the US population having evidence of a duodenal ulcer. The present research aims to find a novel treatment for ethanol induced ulcer by loading thymoquinone (TQ) on a nanostructured lipid carrier (NLC), using Compritol® 888 and coconut oil. The TQ-loaded coconut oil NLC was formulated using melt emulsification combined with a sonication method using Poloxamer 188 as a surfactant. Finally, the optimization of the formulations was performed on a three-factor, three-level Box-Behnken statistical design, with 85.63% entrapment efficiency of TQ in the optimized formulation. A biphasic release pattern of the formulation was recorded in an in vitro drug release study, where the initial burst release of the drug was observed in the first 2 h, followed by a gradual release. Later, the TQ-loaded coconut oil NLC was found to protect the gastric mucous membrane more effectively (78.95% in.; p < 0.01) in an alcohol-induced ulcer model, whereas the TQ suspension showed 30.87% inhibition (p < 0.05) of the ulcerative index, when compared with the ulcer control group. The histopathological evaluations of the stomach in ulcer-induced animals demonstrated protection potential of TQ-loaded coconut oil NLC against an alcohol-induced gastric ulcer. In a nutshell, the entrapment of TQ within the NLC was found to deliver the entrapped drug more effectively when administered through an oral route to possess a gastroprotective effect.

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Section: In Vivo Studymentioning

confidence: 99%

RETRACTED ARTICLE: ArticleNoteOptimization of Thymoquinone-Loaded Coconut Oil Nanostructured Lipid Carriers for the Management of Ethanol-Induced Ulcer

et al. 2020

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“…All the plasma and brain samples were then stored in the biofreezer at À70 C until the analysis of the samples. 33,34…”

Section: Pharmacokinetics Studymentioning

confidence: 99%

Antipsychotic Potential and Safety Profile of TPGS-Based Mucoadhesive Aripiprazole Nanoemulsion: Development and Optimization for Nose-To-Brain Delivery

Kumbhar

Kokare

Shrivastava

et al. 2021

Journal of Pharmaceutical Sciences

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Delivering therapeutics to the brain using conventional dosage forms is always a challenge, thus the present study was aimed to formulate mucoadhesive nanoemulsion (MNE) of aripiprazole (ARP) for intranasal delivery to transport the drug directly to the brain. Therefore, a TPGS based ARP-MNE was formulated and optimized using the Box-Behnken statistical design. The improved in vitro release profile of the formulation was in agreement to enhanced ex vivo permeation through sheep mucous membranes with a maximum rate of permeation co-efficient (62.87 cm h À1 Â 10 3 ) and flux (31.43 mg cm À2 .h À1 ). The pharmacokinetic profile following single-dose administration showed the maximum concentration of drug in the brain (C max ) of 15.19 ± 2.51 mg mL À1 and T max of 1 h in animals with ARP-MNE as compared to 10.57 ± 1.88 mg mL À1 and 1 h, and 2.52 ± 0.38 mg mL À1 and 3 h upon intranasal and intravenous administration of ARP-NE, respectively. Further, higher values of % drug targeting efficiency (96.9%) and % drug targeting potential (89.73%) of ARP-MNE through intranasal administration were investigated. The studies in Wistar rats showed no existence of extrapyramidal symptoms through the catalepsy test and forelimb retraction results. No ex vivo ciliotoxicity on nasal mucosa reflects the safety of the components and delivery tool. Further, findings on locomotor activity and hind-limb retraction test in ARP-MNE treated animals established its antipsychotic efficacy. Thus, it can be inferred that the developed ARP-MNE could effectively be explored as brain delivery cargo in the effective treatment of schizophrenia without producing any toxic manifestation.

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“…A period of 7-10 d was provided to the animals to acclimatize under stipulated laboratory conditions prior to the initiation of experimentation. Throughout the experimental period, animals were housed in polypropylene cages provided by the standard pellet diet (Hindustan Lever Ltd., Mumbai, India) and water ad libitum [12].…”

Section: Animalsmentioning

confidence: 99%

A Controlled Release Microsphere Formulation of an Anti-Diabetic Drug and Characterization of the Microsphere

Chakra

Karan

Das

et al. 2018

Int J Pharm Pharm Sci

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Objective:Here the objective of this study was to prepare and characterize sustained release metformin loaded microsphere formulation which was prepared by W1/O/W2 emulsion solvent evaporation technique. Methods:Guar gum and sodium alginate were used as a matrix building material, whereas ethyl cellulose was applied as a coating polymer. Here various formulations were prepared by changing the drug and guar gum ratio, and the subsequent drug entrapment efficiency (DEE) and drug release were compared and evaluated.Results: Scanning Electron Microscopy (SEM) studies revealed spherical particles with a smooth appearance. Fourier-transform infrared spectroscopy (FTIR) showed there was no interaction between the ingredients in the final formulation. X-ray Diffraction (XRD) studies showed the emergence of polymorphic forms in the final formulation. The drug entrapment in the final drug loaded microsphere formulations was varied from 30-66.78%. The drug release studies showed the continuous release of the drug through twelve hours. The optimized formulation (f2) found to release 71.5% of drugs at the end of the 12th hour following zero order release kinetics. Conclusion:The increase in gum concentration in the W1 phase, which enhances viscosity in the W1 phase, resulting in an increase in the drug entrapment up to an optimum level and a decrease in the release rate. So, it can prolong the action. So by using this tool, we can say that metformin loaded microsphere formulation would be a suitable pharmaceutical formulation for the treatment of diabetic patients in modern drug therapy for its prolonged action.

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Comparative biodistribution and safety profiling of olmesartan medoxomil oil-in-water oral nanoemulsion

Cited by 67 publications

References 24 publications

RETRACTED ARTICLE: ArticleNoteOptimization of Thymoquinone-Loaded Coconut Oil Nanostructured Lipid Carriers for the Management of Ethanol-Induced Ulcer

RETRACTED ARTICLE: ArticleNoteOptimization of Thymoquinone-Loaded Coconut Oil Nanostructured Lipid Carriers for the Management of Ethanol-Induced Ulcer

Antipsychotic Potential and Safety Profile of TPGS-Based Mucoadhesive Aripiprazole Nanoemulsion: Development and Optimization for Nose-To-Brain Delivery

A Controlled Release Microsphere Formulation of an Anti-Diabetic Drug and Characterization of the Microsphere

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