Nanoemulsion-based Parenteral Drug Delivery System of Carbamazepine: Preparation, Characterization, Stability Evaluation and Blood-Brain Pharmacokinetics

Tan, Sim Ling; Stanslas, Johnson; Basri, Mahiran; Karjiban, R A Abedi; Kirby, Brian P.; Sani, Dahiru; Basri, Hamidon

doi:10.2174/1567201812666150901112544

Cited by 33 publications

(20 citation statements)

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“…It is important to note that CBZ release was extremely low (<2%) in the coarse emulsions as well as nanoemulsions at very early time points. The CBZ release was lower than anticipated based on the results of previous publications examining emulsified CBZ systems [47][48][49][50][51]. However, the previous studies examined CBZ release under different conditions: (i) CBZ in lower amounts, (ii) different types of oil phase, (iii) higher concentrations of surfactants, and (iv) use of dialysis membranes with large cutoff sizes.…”

Section: Analytical Methodology For Drug Quantificationmentioning

confidence: 68%

Study of In Vitro and In Vivo Carbamazepine Release from Coarse and Nanometric Pharmaceutical Emulsions Obtained via Ultra-High-Pressure Homogenization

et al. 2020

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In the past decade, pharmaceutical nanotechnology has proven to be a promising alternative for improving the physicochemical and biopharmaceutical features for conventional pharmaceutical drug formulations. The goal of this study was to develop, characterize, and evaluate the in vitro and in vivo release of the model drug carbamazepine (CBZ) from two emulsified formulations with different droplet sizes (coarse and nanometric). Briefly, oil-in-water emulsions were developed using (i) Sacha inchi oil, ultrapure water, TweenTM 80, and SpanTM 80 as surfactants, (ii) methyl-paraben and propyl-paraben as preservatives, and (iii) CBZ as a nonpolar model drug. The coarse and nanometric emulsions were prepared by rotor–stator dispersion and ultra-high-pressure homogenization (UHPH), respectively. The in vitro drug release studies were conducted by dialysis, whereas the in vivo drug release was evaluated in New Zealand breed rabbits. The results showed that nanoemulsions were physically more stable than coarse emulsions, and that CBZ had a very low release for in vitro determination (<2%), and a release of 20% in the in vivo study. However, it was found that nanoemulsions could significantly increase drug absorption time from 12 h to 45 min.

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Section: Analytical Methodology For Drug Quantificationmentioning

confidence: 68%

Study of In Vitro and In Vivo Carbamazepine Release from Coarse and Nanometric Pharmaceutical Emulsions Obtained via Ultra-High-Pressure Homogenization

et al. 2020

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“…There are abundant merits for nanoemulsion-based delivery systems over other dosage forms, such as high surface area, unique transparent appearance, tunable rheology, good stability and bioavailability, and rapid and efficient penetration of the drug moiety [111-118]. Nanoemulsion is currently employed as an important drug carrier in the development of drug formulations for providing pharmaceutically accepted ingredients [112, 119-121].…”

Section: Integration Of Drug Carriers In Microfluidic Platformsmentioning

confidence: 99%

Recent advances of controlled drug delivery using microfluidic platforms

Sanjay

Zhou

Dou

et al. 2018

Advanced Drug Delivery Reviews

278

163

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Conventional systematically-administered drugs distribute evenly throughout the body, get degraded and excreted rapidly while crossing many biological barriers, leaving minimum amounts of the drugs at pathological sites. Controlled drug delivery aims to deliver drugs to the target sites at desired rates and time, thus enhancing the drug efficacy, pharmacokinetics, and bioavailability while maintaining minimal side effects. Due to a number of unique advantages of the recent microfluidic lab-on-a-chip technology, microfluidic lab-on-a-chip has provided unprecedented opportunities for controlled drug delivery. Drugs can be efficiently delivered to the target sites at desired rates in a well-controlled manner by microfluidic platforms via integration, implantation, localization, automation, and precise control of various microdevice parameters. These features accordingly make reproducible, on-demand, and tunable drug delivery become feasible. On-demand self-tuning dynamic drug delivery systems have shown great potential for personalized drug delivery. This review presents an overview of recent advances in controlled drug delivery using microfluidic platforms. The review first briefly introduces microfabrication techniques of microfluidic platforms, followed by detailed descriptions of numerous microfluidic drug delivery systems that have significantly advanced the field of controlled drug delivery. Those microfluidic systems can be separated into four major categories, namely drug carrier-free micro-reservoir-based drug delivery systems, highly integrated carrier-free microfluidic lab-on-a-chip systems, drug carrier-integrated microfluidic systems, and microneedles. Microneedles can be further categorized into five different types, i.e. solid, porous, hollow, coated, and biodegradable microneedles, for controlled transdermal drug delivery. At the end, we discuss current limitations and future prospects of microfluidic platforms for controlled drug delivery.

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“…The polysorbate 80 based nanoemulsion increased the brain bioavailability up to 7.4 folds than the other formulations. 104 Similarly, Tan et al (2015) also used parenteral nanoemulsion for brain targeting of carbamazepine to treat seizure and evaluated its pharmacokinetic efficiency. The study shows higher pharmacokinetic profile and lower side effects of the drug when delivered as nanoemulsion than the free drug solution which assures the potency of carrier system.…”

Section: Nanoemulsionmentioning

confidence: 99%

“…The study shows higher pharmacokinetic profile and lower side effects of the drug when delivered as nanoemulsion than the free drug solution which assures the potency of carrier system. 105 From the available research work, it can be concluded that mucoadhesive nanoemulsion mostly intended for parenteral and intranasal administration to the brain was extensively studied and found as promising carrier system which reduces the associated adverse effect, improves the therapeutic potency and offers a non-invasive patient-friendly technique to access the brain. 106…”

Section: Nanoemulsionmentioning

confidence: 99%

<p>Recent expansions of novel strategies towards the drug targeting into the brain</p>

Alexander¹,

Agrawal²,

Uddin³

et al. 2019

IJN

118

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The treatment of central nervous system (CNS) disorders always remains a challenge for the researchers. The presence of various physiological barriers, primarily the blood–brain barrier (BBB) limits the accessibility of the brain and hinders the efficacy of various drug therapies. Hence, drug targeting to the brain, particularly to the diseased cells by circumventing the physiological barriers is essential to develop a promising therapy for the treatment of brain disorders. Presently, the investigations emphasize the role of different nanocarrier systems or surface modified target specific novel carrier system to improve the efficiency and reduce the side effects of the brain therapeutics. Such approaches supposed to circumvent the BBB or have the ability to cross the barrier function and thus increases the drug concentration in the brain. Although the efficacy of novel carrier system depends upon various physiological factors like active efflux transport, protein corona of the brain, stability, and toxicity of the nanocarrier, physicochemical properties, patient-related factors and many more. Hence, to develop a promising carrier system, it is essential to understand the physiology of the brain and BBB and also the other associated factors. Along with this, some alternative route like direct nose-to-brain drug delivery can also offer a better means to access the brain without exposure of the BBB. In this review, we have discussed the role of various physiological barriers including the BBB and blood-cerebrospinal fluid barrier (BCSFB) on the drug therapy and the mechanism of drug transport across the BBB. Further, we discussed different novel strategies for brain targeting of drug including, polymeric nanoparticles, lipidic nanoparticles, inorganic nanoparticles, liposomes, nanogels, nanoemulsions, dendrimers, quantum dots, etc. along with the intranasal drug delivery to the brain. We have also illustrated various factors affecting the drug targeting efficiency of the developed novel carrier system.

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Nanoemulsion-based Parenteral Drug Delivery System of Carbamazepine: Preparation, Characterization, Stability Evaluation and Blood-Brain Pharmacokinetics

Cited by 33 publications

References 0 publications

Study of In Vitro and In Vivo Carbamazepine Release from Coarse and Nanometric Pharmaceutical Emulsions Obtained via Ultra-High-Pressure Homogenization

Study of In Vitro and In Vivo Carbamazepine Release from Coarse and Nanometric Pharmaceutical Emulsions Obtained via Ultra-High-Pressure Homogenization

Recent advances of controlled drug delivery using microfluidic platforms

<p>Recent expansions of novel strategies towards the drug targeting into the brain</p>

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