Formulation Optimization of a Palm-Based Nanoemulsion System Containing Levodopa

Zainol, Syafinaz; Basri, Mahiran; Basri, Hamidon; Shamsuddin, Ahmad Fuad; Abdul-Gani, Siti Salwa; Karjiban, Roghayeh Abedi; Abdulmalek, Emilia

doi:10.3390/ijms131013049

Cited by 88 publications

(80 citation statements)

References 27 publications

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“…Figure 9F and G shows that the combination of increased mixing rate and water content and the combination of increased mixing rate and addition rate widened the droplet-size distribution of the final emulsion. These results are well supported by previous reports 18,24 on high-pressure emulsification processes. Conversely, Figure 9D shows that the combination of increased water content and addition rate narrow droplet-size distribution.…”

Section: Polydispersity Indexsupporting

confidence: 82%

Formulation, development, and optimization of a novel octyldodecanol-based nanoemulsion for transdermal delivery of ceramide IIIB

Su¹,

Yang²,

Wang³

et al. 2017

IJN

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This research aimed to develop and optimize a nanoemulsion-based formulation containing ceramide IIIB using phase-inversion composition for transdermal delivery. The effects of ethanol, propylene glycol (PG), and glycerol in octyldodecanol and Tween 80 systems on the size of the nanoemulsion region in the phase diagrams were investigated using water titration. Subsequently, ceramide IIIB loading was kept constant (0.05 wt%), and the proposed formulation and conditions were optimized via preliminary screening and experimental design. Factors such as octyldodecanol/(Tween 80:glycerol) weight ratio, water content, temperature, addition rate, and mixing rate were investigated in the preliminary screening experiment. Response surface methodology was employed to study the effect of water content (30%–70%, w/w), mixing rate (400–720 rpm), temperature (20°C–60°C), and addition rate (0.3–1.8 mL/min) on droplet size and polydispersity index. The mathematical model showed that the optimum formulation and conditions for preparation of ceramide IIIB nanoemulsion with desirable criteria were a temperature of 41.49°C, addition rate of 1.74 mL/min, water content of 55.08 wt%, and mixing rate of 720 rpm. Under optimum formulation conditions, the corresponding predicted response values for droplet size and polydispersity index were 15.51 nm and 0.12, respectively, which showed excellent agreement with the actual values (15.8 nm and 0.108, respectively), with no significant ( P >0.05) differences.

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Section: Polydispersity Indexsupporting

confidence: 82%

Formulation, development, and optimization of a novel octyldodecanol-based nanoemulsion for transdermal delivery of ceramide IIIB

Su¹,

Yang²,

Wang³

et al. 2017

IJN

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“…Mathematical modeling offers a valuable tool for formulation optimization, by facilitating an integrated and quantitative assessment of the outcome of various formulation attributes on the response parameter(s) of interest, without the need to experimentally test each individual scenario. Studies by Zainol et al, illustrate the utility of the Response Surface Methodology in optimizing Levodopa Palm-based nanoemulsions (17): these authors were able to successfully predict the effects of varying the formulation composition and manufacturing process on three nanoemulsion variables: particle size, zeta potential and polydispersity index. Although this process is empirical, it nonetheless highlights the benefits of applying mathematical modeling to formulation optimization efforts.…”

Section: Introductionmentioning

confidence: 99%

Mathematical Modeling and Experimental Validation of Nanoemulsion-Based Drug Transport across Cellular Barriers

2017

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Purpose Nanoemulsions have shown potential in delivering drug across epithelial and endothelial cell barriers, which express efflux transporters. However, their transport mechanisms are not entirely understood. Our goal was to investigate the cellular permeability of nanoemulsion-encapsulated drugs and apply mathematical modeling to elucidate transport mechanisms and sensitive nanoemulsion attributes. Methods Transport studies were performed in Caco-2 cells, using fish oil nanoemulsions and a model substrate, rhodamine-123. Permeability data was modeled using a semi-mechanistic approach, capturing the following cellular processes: endocytotic uptake of the nanoemulsion, release of rhodamine-123 from the nanoemulsion, efflux and passive permeability of rhodamine-123 in aqueous solution. Results Nanoemulsions not only improved the permeability of rhodamine-123, but were also less sensitive to efflux transporters. The model captured bidirectional permeability results and identified sensitive processes, such as the release of the nanoemulsion-encapsulated drug and cellular uptake of the nanoemulsion. Conclusions Mathematical description of cellular processes, improved our understanding of transport mechanisms, such as nanoemulsions don’t inhibit efflux to improve drug permeability. Instead, their endocytotic uptake, results in higher intracellular drug concentrations, thereby increasing the concentration gradient and transcellular permeability across biological barriers. Modeling results indicated optimizing nanoemulsion attributes like the droplet size and intracellular drug release rate, may further improve drug permeability.

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“…Many studies have been reported the lipid nano-emulsions as a parenteral drug delivery device. These nano-emulsions can circulate in the blood for long period of time (Anuchapreeda et al, 2012) and minimize the pain by exposing the tissue to lower concentrations of drugs (Zainol et al, 2012). Furthermore, PKOEs with relatively shorter chain ester are potentially good for delivery of drug into the body (Keng et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

Computational simulation of palm kernel oil-based esters nano-emulsions aggregation as a potential parenteral drug delivery system

Faujan

Karjiban

Kashaban

et al. 2019

Arabian Journal of Chemistry

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The self-assembled structure of palm kernel oil-based esters (PKOEs) nano-emulsions has shown a great potential used for parenteral drug delivery applications. Here, all-atom level molecular dynamics (MD) was applied to investigate the aggregation process of PKOEs nano-emulsion system. The system consisted of palm kernel oil-based esters (PKOEs) and dipalmitoylphosphatidylcholine (DPPC) in water. The ratio of all constituents was taken from the homogenous region of a ternary phase diagram determined experimentally. The molecules started to aggregate very rapidly from random configurations. A doughnut-like toroidal assembled structure formed at 50 ns with PKOEs surrounded by DPPC molecules. The structural and dynamical properties of the self-assembled doughnut-like toroidal aggregate were analyzed using the principle moment of inertia, eccentricity and radius of gyration. The aggregation structures were compact with the average radius of gyration of 4.10 (±0.02) nm over the last 5 ns. Additionally, both hydrophobic

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Formulation Optimization of a Palm-Based Nanoemulsion System Containing Levodopa

Cited by 88 publications

References 27 publications

Formulation, development, and optimization of a novel octyldodecanol-based nanoemulsion for transdermal delivery of ceramide IIIB

Formulation, development, and optimization of a novel octyldodecanol-based nanoemulsion for transdermal delivery of ceramide IIIB

Mathematical Modeling and Experimental Validation of Nanoemulsion-Based Drug Transport across Cellular Barriers

Computational simulation of palm kernel oil-based esters nano-emulsions aggregation as a potential parenteral drug delivery system

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