Exploring oral nanoemulsions for bioavailability enhancement of poorly water-soluble drugs

Kotta, Sabna; Khan, Abdul Wadood; Pramod, K.; Ansari, S. H.; Sharma, Rakesh Kumar; Ali, Javed

doi:10.1517/17425247.2012.668523

Cited by 151 publications

(72 citation statements)

References 62 publications

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“…27 Similarly, the active components encapsulated within NE droplets can be protected from oxidation, hydrolysis, and volatilization. 28 High-and low-energy approaches constitute the two major methods for formulating NE. 29,30 In industry, the formulation of NE is performed using the high-energy approach, which utilizes mechanical devices capable of generating intense disruptive forces that break up the oil and water phases, leading to the formation of tiny oil droplets.…”

Section: Introductionmentioning

confidence: 99%

Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide

Yen

Chen

et al. 2018

IJN

104

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Background Andrographolide (AG), a compound with low water solubility, possesses various pharmacological activities, particularly anti-inflammatory activity. However, its low oral bioavailability is a major obstacle to its potential use. This study developed and optimized an AG-loaded nanoemulsion (AG-NE) formulation to improve AG oral bioavailability and its protective effects against inflammatory bowel disease. Methods A high-pressure homogenization technique was used to prepare the AG-NE and solubility, viscosity, and droplet size tests were conducted to develop the optimized AG-NE composed of α-tocopherol, ethanol, Cremophor EL, and water. The permeability was assessed using everted rat gut sac method and in vivo absorption and anti-inflammatory effect in rats was also evaluated. The plasma concentration of AG was determined using our validated high performance liquid chromatography method, which was used to generate a linear calibration curve over the concentration range of 0.1–25 μg/mL in rat plasma ( R 2 >0.999). Results The optimized AG-NE had a droplet size of 122±11 nm confirmed using transmission electron microscopy and a viscosity of 28 centipoise (cps). It was stable at 4 and 25°C for 90 days. An ex vitro intestinal permeability study indicated that the jejunum was the optimal site for AG absorption from the optimized AG-NE, which was 8.21 and 1.40 times higher than that from an AG suspension and AG ethanol solution, respectively. The pharmacokinetic results indicate that the absorption of AG from AG-NE was significantly enhanced in comparison with that from the AG suspension, with a relative bioavailability of 594.3%. Moreover, the ulcer index and histological damage score of mice with indomethacin-induced intestinal lesions were significantly reduced by AG-NE pretreatment. Conclusion We conclude that the developed AG-NE not only enhanced the oral bioavailability of AG in this study but may also prove to be an effective formulation of AG for preventing gastrointestinal inflammatory disorders.

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Section: Introductionmentioning

confidence: 99%

Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide

Yen

Chen

et al. 2018

IJN

104

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“…28 Though these theories represent completely different flow regimes and were developed for macroemulsions, many modern nanoemulsion studies have referred to Taylor's theory as well as Hinze's theory to explain trends observed in droplet size. 2,17,18,20,23,[29][30][31][32][33][34][35][36][37] However, few studies also acknowledge that the agreement with Taylor's and Hinze's theory is only qualitative at best and that these theories should be used only for an order of magnitude estimation of droplet size. 17,23 Further, there are also experimental studies on nanoemulsion which do not use any theoretical prediction and fit their droplet size data using empirical power law correlations.…”

Section: Introductionmentioning

confidence: 99%

Controlling and predicting droplet size of nanoemulsions: scaling relations with experimental validation

et al. 2016

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a Nanoemulsions possess powerful nano-scale properties that make them attractive for diverse applications such as drug delivery, food supplements, nanoparticle synthesis and pharmaceutical formulation. However, there is little knowledge in nanoemulsion literature about controlling and predicting droplet size. In this article, we propose a scaling relation to predict the dependence of nanoemulsion droplet size with physical properties such as viscosity of the droplet phase and continuous phase, and process parameters such as input power density. We validate our proposed scaling with a wide range of droplet size data from nanoemulsions prepared with high pressure homogenization and ultrasonication. Our proposed scaling also compares favorably with experimental data from literature. The scaling relation can serve as a guiding principle for rational design of nanoemulsions.

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“…In addition, as far as the method for improving solubility is concerned, molecular inclusion complexation technology might be equally or more effective and much simpler and easier for production scale-up than other approaches, such as emulsification and phospholipid complexation. 25,26 Formation of RAABCD was confirmed by differential scanning calorimetry and FTIR spectroscopy. As shown in Figure 3A, the differential scanning calorimetry thermogram for rifaldazine showed a sharp peak at 259°C, corresponding to the melting point of rifaldazine.…”

Section: Preparation and Characterization Of Raabcdmentioning

confidence: 93%

Characterization, activity, and computer modeling of a molecular inclusion complex containing rifaldazine

Tan¹,

He²,

Wu³

et al. 2013

IJN

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Background:The purpose of this study was to develop, characterize, and investigate a molecular inclusion complex containing rifaldazine with good solubility and antibacterial activity. Methods: Rifaldazine, a lipophilic molecule, was encapsulated into the hydrophobic cavity of β-cyclodextrin to form a molecular inclusion complex (RAABCD) with good solubility. RAABCD was prepared in a short time using a solid-state grinding method. The inclusion ratio, binding constant, and change in Gibbs free energy were determined by a phase solubility diagram and/or ultraviolet-visible spectroscopy. Differential scanning calorimetry and Fourier transform infrared spectroscopy of RAABCD were performed. Morphological features of RAABCD were observed by photomicroscopy. The most likely optimal configuration for RAABCD was simulated by computer modeling. Broth macrodilution testing was done to investigate the antibacterial activity of RAABCD. Results: The inclusion ratio, binding constant, and change in Gibbs free energy, determined by a phase solubility diagram and/or ultraviolet-visible spectroscopy were 1:1, 288.33/261.33 L/mol, and 32.29/31.73 kJ/mol, respectively. Differential scanning calorimetry and Fourier transformed infrared spectra of RAABCD confirmed the molecular interaction between rifaldazine and β-cyclodextrin. The morphological difference between irregular and amorphous-shaped RAABCD and columnar-shaped rifaldazine further confirmed the molecular encapsulation of rifaldazine. The most likely optimal configuration for RAABCD was confirmed by computer modeling. Broth macrodilution testing indicated that RAABCD had good antibacterial activity. Conclusion: RAABCD had improved solubility and good activity, and might be a promising alternative for treatment of a range of bacterial infections.

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Exploring oral nanoemulsions for bioavailability enhancement of poorly water-soluble drugs

Abstract: Low-energy emulsification techniques can also produce stable nanoemulsions. It is guaranteed that oral nanoemulsions can act as a potential tool for the delivery of poorly water-soluble therapeutic moieties in a very efficient manner.

Cited by 151 publications

References 62 publications

Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide

Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide

Controlling and predicting droplet size of nanoemulsions: scaling relations with experimental validation

Characterization, activity, and computer modeling of a molecular inclusion complex containing rifaldazine

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