Potentials and challenges in self-nanoemulsifying drug delivery systems

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

doi:10.1517/17425247.2012.719870

Cited by 98 publications

(63 citation statements)

References 65 publications

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“…Novel self-emulsifying drug delivery systems (SEDDS) have received considerable attention due to their capability of improving oral absorption of highly hydrophobic compounds [36,37]. SEDDS formulations are isotropic mixture of oils, surfactants, nutrients (or drugs), usually with one or more of co-surfactants or co-emulsifiers [32,36].…”

Section: Biocompatible and Biodegradable Nanoparticlesmentioning

confidence: 99%

Application of nanotechnology in improving bioavailability and bioactivity of diet-derived phytochemicals

Wang

Nie

et al. 2014

The Journal of Nutritional Biochemistry

410

245

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Nanotechnology is an innovative approach that has potential applications in nutraceutical research. Phytochemicals have promising potential for maintaining and promoting health, as well as preventing and potentially treating some diseases. However, the generally low solubility, stability, bioavailability and target specificity, together with the side-effects seen when used at high levels, have limited their application. Indeed, nanoparticles can increase solubility and stability of phytochemicals, enhance their absorption, protect them from premature degradation in the body, and prolong their circulation time. Moreover, these nanoparticles exhibit high differential uptake efficiency in the target cells (or tissue) over normal cells (or tissue)through preventing them from prematurely interacting with the biological environment, enhanced permeation and retention effect in disease tissues, and improving their cellular uptake, resulting in decreased toxicity, In this review we outline the commonly used biocompatible and biodegradable nanoparticles including liposomes, emulsions, solid lipid nanoparticles, nanostructured lipid carriers, micelles and poly (lactic-co-glycolic acid) (PLGA) nanoparticles. We then summarize studies that have used these nanoparticles as carriers for EGCG, quercetin, resveratrol and curcuminadministration to enhance their aqueous solubility, stability, bioavailability, target specificity, and bioactivities.

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Section: Biocompatible and Biodegradable Nanoparticlesmentioning

confidence: 99%

Application of nanotechnology in improving bioavailability and bioactivity of diet-derived phytochemicals

Wang

Nie

et al. 2014

The Journal of Nutritional Biochemistry

410

245

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“…Tea tree oil contains more than 100 chemical compounds, especially monoterpenes and alcohol-bound sesquiterpenes [4]. The main component in this oil is terpinen-4-ol, which exhibits antibacterial activity [5,6]. However, the hydrophobic properties of tea tree oil cause solubility problems in water-based preparations.…”

Section: Introductionmentioning

confidence: 99%

Studies on the Formulation, Physical Stability, and in Vitro Antibacterial Activity of Tea Tree Oil (Melaleuca Alternifolia) Nanoemulsion Gel

2017

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Objective: This study aimed to formulate tea tree oil into a nanoemulsion gel dosage form and evaluate its physical stability and antibacterial activity.Methods: Nanoemulsion gels were formulated with various concentrations of tea tree oil, namely, 5%, 7%, and 9%, using Tween-80 as a surfactant and propylene glycol as a cosurfactant. The tea tree oil nanoemulsion gels showed a stable physical appearance over 8 weeks of storage at low temperature (4±2°C) and room temperature (25±2°C), cycling test, and centrifugation test. Results:The best formula was nanoemulsion gel formulation 1 (F1), which contained 5% tea tree oil, due to its good stability, smaller globule size, and greater viscosity. The results for antibacterial activity, determined by in vitro study, showed that the tea tree oil nanoemulsion gels exhibited antibacterial activity against Propionibacterium acnes through the formation of an inhibition zone. Conclusion:Higher concentrations of tea tree oil in nanoemulsion gels (5%, 7%, and 9%) showed greater mean inhibition zones (28.33±0.88 mm, 30.33±0.33 mm, and 31.67±0.33 mm, respectively).

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“…Therefore, we infer that RTV ISNPs and RTV NPs are very likely a similar type of NPs. Unlike self-emulsifying microemulsions and nanoemulsions, 10 RTV ISNPs were stable for changes of environment, RTV was kept inside the ISNPs over the period of the release study, and there was no RTV precipitation after RTV ISNPs were diluted over 1,000 times. With this novel ISNP nanotechnology, we achieved over 16% drug loading of RTV in RTV ISNP granules, which could provide a dose of about 100 mg per administration in humans.…”

Section: Discussionmentioning

confidence: 99%

“…Considering oral solid dosage forms are preferred for stability, manufacturing, storage, and transportation, lipid-based NPs have limited applications for oral medications. 7,10 To address the issue, research efforts were directed toward converting liquid formulations into solid forms. However, low drug loading in the final solid forms was often obtained, as great amounts of solid excipients had to be added to remove water and/or achieve good flow properties.…”

mentioning

confidence: 99%

Novel in situ self-assembly nanoparticles for formulating a poorly water-soluble drug in oral solid granules, improving stability, palatability, and bioavailability

Guo

Pham

et al. 2016

IJN

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Purpose The purpose of this study was to develop a novel lipid-based nanotechnology to formulate poorly water-soluble drugs in oral solid granules to improve stability, palatability, and bioavailability. Materials and methods In one method, we prepared ritonavir (RTV) nanoparticles (NPs) by a microemulsion-precursor method and then converted the RTV NPs to solid granules by wet granulation to produce RTV NP-containing granules. In the other innovative method, we did not use water in the formulation preparation, and discovered novel in situ self-assembly nanoparticles (ISNPs). We prepared RTV ISNP granules that did not initially contain NPs, but spontaneously produced RTV ISNPs when the granules were introduced to water with gentle agitation. We fully characterized these RTV nanoformulations. We also used rats to test the bioavailability of RTV ISNP granules. Finally, an Astree electronic tongue was used to assess the taste of the RTV ISNP granules. Results RTV NP-containing granules only had about 1% drug loading of RTV in the solid granules. In contrast, RTV ISNP granules achieved over 16% drug loading and were stable at room temperature over 24 weeks. RTV ISNPs had particle size between 160 nm and 300 nm with narrow size distribution. RTV ISNPs were stable in simulated gastric fluid for 2 hours and in simulated intestinal fluid for another 6 hours. The data from the electronic tongue showed that the RTV ISNP granules were similar in taste to blank ISNP granules, but were much different from RTV solution. RTV ISNP granules increased RTV bioavailability over 2.5-fold compared to RTV solution. Conclusion We successfully discovered and developed novel ISNPs to manufacture RTV ISNP granules that were reconstitutable, stable, and palatable, and improved RTV bioavailability. The novel ISNP nanotechnology is a platform to manufacture oral solid dosage forms for poorly water-soluble drugs, especially for pediatric formulation development.

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Potentials and challenges in self-nanoemulsifying drug delivery systems

Cited by 98 publications

References 65 publications

Application of nanotechnology in improving bioavailability and bioactivity of diet-derived phytochemicals

Application of nanotechnology in improving bioavailability and bioactivity of diet-derived phytochemicals

Studies on the Formulation, Physical Stability, and in Vitro Antibacterial Activity of Tea Tree Oil (Melaleuca Alternifolia) Nanoemulsion Gel

Novel in situ self-assembly nanoparticles for formulating a poorly water-soluble drug in oral solid granules, improving stability, palatability, and bioavailability

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Potentials and challenges in self-nanoemulsifying drug delivery systems

Cited by 98 publications

References 65 publications

Application of nanotechnology in improving bioavailability and bioactivity of diet-derived phytochemicals

Application of nanotechnology in improving bioavailability and bioactivity of diet-derived phytochemicals

Studies on the Formulation, Physical Stability, and in Vitro Antibacterial Activity of Tea Tree Oil (Melaleuca Alternifolia) Nanoemulsion Gel

Novel in situ self-assembly nanoparticles for formulating a poorly water-soluble drug in oral solid granules, improving stability, palatability, and&nbsp;bioavailability

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Novel in situ self-assembly nanoparticles for formulating a poorly water-soluble drug in oral solid granules, improving stability, palatability, and bioavailability