Anti HIV nanoemulsion formulation: Optimization and in vitro–in vivo evaluation

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

doi:10.1016/j.ijpharm.2013.12.038

Cited by 52 publications

(31 citation statements)

References 20 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A surfactant or emulsifying agent is important in formulating a nanoemulsion because it reduces interfacial energy between oil and the aqueous phase via formation of a layer around the droplets of the nanoemulsion and it provides a mechanical barrier to coalescence (Kotta et al, 2014). Hence, surfactants added to a water-in-oil system (nutmeg oil, water, and glycerol) increase the aqueous phase concentration due to micelle solubilization.…”

Section: Results and Discussion Phase Diagram For Ntsmentioning

confidence: 99%

Biocompatible Nutmeg Oil-Loaded Nanoemulsion as Phyto-Repellent

et al. 2020

View full text Add to dashboard Cite

Plant essential oils are widely used in perfumes and insect repellent products. However, due to the high volatility of the constituents in essential oils, their efficacy as a repellent product is less effective than that of synthetic compounds. Using a nanoemulsion as a carrier is one way to overcome this disadvantage of essential oils. Nutmeg oil-loaded nanoemulsion (NT) was prepared using a high speed homogenizer and sonicator with varying amounts of surfactant, glycerol, and distilled water. Using a phase diagram, different formulations were tested for their droplet size and insect repellent activity. The nanoemulsion containing 6.25% surfactant and 91.25% glycerol (NT 6) had the highest percentage of protection (87.81%) in terms of repellent activity among the formulations tested for the 8 h duration of the experiment. The droplet size of NT 6 was 217.4 nm, and its polydispersity index (PDI) was 0.248. The zeta potential value was-44.2 mV, and the viscosity was 2.49 Pa.s at pH 5.6. The in vitro release profile was 71.5%. When the cytotoxicity of NT 6 at 400 µg/mL was tested using the MTS assay, cell viability was 97.38%. Physical appearance and stability of the nanoemulsion improved with the addition of glycerol as a co-solvent. In summary, a nutmeg oil-loaded nanoemulsion was successfully formulated and its controlled release of the essential oil showed mosquito repellent activity, thus eliminating the disadvantages of essential oils.

show abstract

Section: Results and Discussion Phase Diagram For Ntsmentioning

confidence: 99%

Biocompatible Nutmeg Oil-Loaded Nanoemulsion as Phyto-Repellent

et al. 2020

View full text Add to dashboard Cite

show abstract

“…In the same way, the free drug presents a behavior, which is typical from a dispersed system, considering a low aqueous soluble drug. 33) In the case of the nanoemulsion, both of sustained release 34,35) and rapid release 36) as compared with the drug suspension were reported. In the present study, the release profiles indicate that morin was incorporated into the border between the oil phase and surfactants and was gradually released from dispersed droplets by diffusion at a similar diffusion rate to that of the morin suspension.…”

Section: Discussionmentioning

confidence: 99%

Influence of Polysorbate 60 on Formulation Properties and Bioavailability of Morin-Loaded Nanoemulsions with and without Low-Saponification-Degree Polyvinyl Alcohol

Ikeuchi-Takahashi

Kobayashi

Ishihara

et al. 2018

Biological & Pharmaceutical Bulletin

View full text Add to dashboard Cite

The aim of the present study was to investigate the influence of polysorbate 60 (Tween 60) on the development of morin-loaded nanoemulsions to improve the oral bioavailability of morin. Nanoemulsions were prepared using Tween 60 and polyvinyl alcohol (PVA) as emulsifiers, and medium chain triglycerides (MCT) as the lipid base. Low-saponification-degree PVA (LL-810) was also added to stabilize dispersed droplets. MCT-LL810 nanoemulsion containing LL-810 was prepared with a reduced amount of Tween 60. However, the area under the blood concentration-time curve (AUC) of MCT-LL810 (0.18) nanoemulsion containing a small amount of Tween 60 did not increase because the absorption of morin was limited by P-glycoprotein (P-gp)-mediated efflux. MCT-LL810 (0.24) nanoemulsion containing a large amount of Tween 60 showed the highest AUC, dispersed droplets containing Tween 60 may have been transported into epithelial cells in the small intestine, and P-gp transport activity appeared to be suppressed by permeated Tween 60. Based on the plasma concentration profile, dispersed droplets in MCT-LL810 (0.24) nanoemulsion permeated more rapidly through the mucus layer and the intestinal membrane than MCT (0.24) nanoemulsion without LL-810. In conclusion, a novel feature of Tween 60 incorporated into the dispersed droplets of a nanoemulsion interacting with P-gp was demonstrated herein. Dispersed droplets in MCT-LL810 (0.24) nanoemulsion containing LL-810 permeated rapidly through the mucus layer and intestinal membrane, and Tween 60 incorporated in dispersed droplets interacted with P-gp-mediated efflux, increasing the bioavailability of morin.Key words nanoemulsion; morin; polyvinyl alcohol; bioavailability; P-glycoprotein Morin (2′,4′,3,5,7-pentahydroxyflavonoid) is one of the flavonoids widely found in fruits, vegetables, tea, and numerous therapeutic herbs.1) Its wide spectrum of biological activities, including anti-inflammatory, anti-cancer, antioxidant, antiangiogenic, anti-hypertensive, and anti-clastogenic activities, have been reported. [2][3][4][5][6][7][8] We previously demonstrated that a treatment with morin induced basal nitric oxide production and rapid improvements in endothelial function in diabetic mice.9) Morin has been suggested to improve the development of endothelial dysfunction by diabetes. However, the absolute bioavailability of morin after its oral administration is very low (less than 1%), and this may be attributed to its low aqueous solubility, P-glycoprotein (P-gp)-mediated efflux, and low intestinal permeability. [10][11][12] Various approaches have been attempted in order to increase the area under the blood concentration-time curve (AUC) of low bioavailability drugs after their oral administration. Nanoemulsion systems have received increasing attention as appropriate carriers for insoluble active compounds to increase bioavailability and modify drug release characteristics. [13][14][15] Improvements in the solubility of drugs into nanoemulsion components such as the oil phase and surfactants repre...

show abstract

“…Approximately 2 min after sample deposition, the grid was tapped with filter paper to remove surface water and air-dried. The image was taken with transmission electron microscope at an acceleration voltage of 100 KV [20,23].…”

Section: Transmission Electron Microscopy (Tem)mentioning

confidence: 99%

“…A 1 ml of the aliquots was withdrawn at predetermined time intervals, (5, 15, 30, 45 and 60 min) from the dissolution medium and replaced with fresh blank media. The withdrawn samples were filtered using 0.45 mm Millipore filter and analyzed for drug content by UV-vis spectrophotometer (UV-1800, Shimadzu, Japan) using the corresponding blank medium at 317 nm [22,23,25].…”

Section: In Vitro Drug Releasementioning

confidence: 99%

Prototype Self Emulsifying System of Etravirine: Design, Formulation and in Vitro Evaluation

Preethi

Shivakumar

Kumar³

et al. 2018

Int J App Pharm

View full text Add to dashboard Cite

Objective: Lipid-based formulations have gained much attention, particularly on self-emulsifying drug delivery systems (SEDDS), to improve the oral bioavailability of lipophilic drugs. In the present study, an attempt was made to develop and evaluate prototype SEDDS of poorly soluble antiviral BCS class IV drug etravirine.Methods: Various oils, surfactants and co-surfactants were screened for their suitability in the formulation of SEDDS. Based on the screening, gelucire 44/14, as the oil, labrasol as a surfactant and transcutol HP as the co-surfactant were selected. SEDDS with drug etravirine was formulated and evaluated for emulsifying ability, dilution potential and microscopic properties. The emulsion area for each of the combination of oil and surfactant co-surfactant mixture (Smix) was determined by the construction of pseudo-ternary phase diagrams.Results: The optimized formulation with oil (gelucire 44/14) and Smix (labrasol: transcutol HP, 6:1) in a ratio of 2:8 exhibited a rapid emulsification rate and a good polydispersibility index of 0.103±0.012 indicating uniformity of the formed droplets. The size of the droplets was determined by zetasizer and was found to be in 200 nm range. The drug release from the final formulation after 2hr was found to be 41.15%±0.5 compared to 19.3%±3.8 of pure drug indicating enhanced dissolution profile of the drug.Conclusion: In vitro study illustrated enhanced dissolution rate of formulated prototype SEDDS of BCS class IV drug etravirine for oral delivery.

show abstract

Anti HIV nanoemulsion formulation: Optimization and in vitro–in vivo evaluation

Cited by 52 publications

References 20 publications

Biocompatible Nutmeg Oil-Loaded Nanoemulsion as Phyto-Repellent

Biocompatible Nutmeg Oil-Loaded Nanoemulsion as Phyto-Repellent

Influence of Polysorbate 60 on Formulation Properties and Bioavailability of Morin-Loaded Nanoemulsions with and without Low-Saponification-Degree Polyvinyl Alcohol

Prototype Self Emulsifying System of Etravirine: Design, Formulation and in Vitro Evaluation

Contact Info

Product

Resources

About