Formulation and characterization of self-nanoemulsifying drug delivery systems containing monoacyl phosphatidylcholine

Tran, Thuy Linh; Xi, Xi; Rades, Thomas

doi:10.1016/j.ijpharm.2016.02.026

Cited by 27 publications

(9 citation statements)

References 27 publications

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“…The surface zeta potential plays a significant role in stabilizing the nanoformulations. Generally, the value of zeta potential above 20 is an indicator of stabilized formulation as it results in higher repulsive force between the globules and ruling out the possibility of coalescence [8]. In view of these results, formulation LCT 14 was found to be the most stable formulation due to inter particulate repulsion allowing them to suspend for a longer period of time [9].…”

Section: Discussionmentioning

confidence: 99%

“…The most popular nano-based strategies for lipophilic drugs include incorporation of drugs in lipid vehicles like oil/surfactant dispersion [5], micro and nanoemulsions [6,7], and self emulsifying drug delivery systems. Self-nanoemulsifying drug delivery systems (SNEDDS) have emerged as a vital strategy for the efficient delivery of drugs with poor aqueous solubility [8,9,10]. SNEDDS are well known for their potential to enhance the solubility and absorption of the lipophilic drugs [11] by increasing the surface area and decreasing the size of oil droplets that are readily digestible and incorporated into mixed micelles that can pass the intestinal lumen [12].…”

Section: Introductionmentioning

confidence: 99%

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Self-Nanoemulsifying Drug Delivery System (SNEDDS) for Improved Oral Bioavailability of Chlorpromazine: In Vitro and In Vivo Evaluation

et al. 2019

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Background and Objectives: Lipid-based self-nanoemulsifying drug delivery systems (SNEDDS) have resurged the eminence of nanoemulsions by modest adjustments and offer many valuable opportunities in drug delivery. Chlorpromazine, an antipsychotic agent with poor aqueous solubility—with extensive first-pass metabolism—can be a suitable candidate for the development of SNEDDS. The current study was designed to develop triglyceride-based SNEDDS of chlorpromazine to achieve improved solubility, stability, and oral bioavailability. Materials and Methods: Fifteen SNEDDS formulations of each short, medium, and long chain, triglycerides were synthesized and characterized to achieve optimized formulation. The optimized formulation was characterized for several in vitro and in vivo parameters. Results: Particle size, zeta potential, and drug loading of the optimized SNEDDS (LCT14) were found to be 178 ± 16, −21.4, and 85.5%, respectively. Long chain triglyceride (LCT14) showed a 1.5-fold increased elimination half-life (p < 0.01), up to 6-fold increased oral bioavailability, and 1.7-fold decreased plasma clearance rate (p < 0.01) compared to a drug suspension. Conclusion: The findings suggest that SNEDDS based on long-chain triglycerides (LCT14) formulations seem to be a promising alternative for improving the oral bioavailability of chlorpromazine.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Self-Nanoemulsifying Drug Delivery System (SNEDDS) for Improved Oral Bioavailability of Chlorpromazine: In Vitro and In Vivo Evaluation

et al. 2019

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“…In the present study, nanoemulsion formulations were used for the encapsulation of three antibiotics including linezolid, doxycycline, and clindamycin, because they are thermodynamically stable solutions and easy to prepare and can solubilize poorly soluble drugs, thus enhancing their bioavailability [14, 36–38].…”

Section: Discussionmentioning

confidence: 99%

In Vitro Evaluation of Antimicrobial Activity and Cytotoxicity of Different Nanobiotics Targeting Multidrug Resistant and Biofilm Forming Staphylococci

Mohamed

Nasr

Elkhatib

et al. 2018

BioMed Research International

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Antibiotic-resistant and biofilm-forming bacteria have surprisingly increased over recent years. On the contrary, the rate of development of new antibiotics to treat these emerging superbugs is very slow. Therefore, the aim of this study was to prepare novel nanobiotic formulations to improve the antimicrobial activity of three antibiotics (linezolid, doxycycline, and clindamycin) against Staphylococci. Antibiotics were formulated as nanoemulsions and evaluated for their antimicrobial activities and cytotoxicities. Cytotoxicity of the conventional antibiotics and nanobiotics was analyzed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on rat hepatocytes. Half-maximal inhibitory concentration (IC50) was estimated from an experimentally derived dose-response curve for each concentration using GraphPad Prism software. Upon quantitative assessment of Staphylococcus biofilm formation, eighty-four isolates (66.14 %) were biofilm forming. Linezolid and doxycycline nanobiotics exhibited promising antibacterial activities. On the contrary, clindamycin nanobiotic exhibited poor antibacterial activity. Minimum biofilm inhibitory concentrations showed that 73.68 %, 45.6%, and 5.2% of isolates were sensitive to linezolid, doxycycline, and clindamycin nanobiotics, respectively. Results of this study revealed that antibiotics loaded in nanosystems had a higher antimicrobial activity and lower cytotoxicities as compared to those of conventional free antibiotics, indicating their potential therapeutic values.

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“…A similar experimental protocol has been previously described. 22 Briefly, before adding lipase extract, 1.00 mL of SNEDDS was predispersed in 36 mL of digestion medium for 5 min in a thermostated vessel maintained at 37 C. The pH of the dispersion was adjusted to 6.5. Adding 4 mL of fresh pancreatic lipase extract (pH 6.5) to the system initiated the lipolysis reaction with an enzyme concentration of approximately 400 USP units/mL.…”

Section: In Vitro Lipolysismentioning

confidence: 99%

Using Potentiometric Free Drug Sensors to Determine the Free Concentration of Ionizable Drugs in Colloidal Systems

Tran

Chakraborty

et al. 2018

Journal of Pharmaceutical Sciences

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The present study investigates the use of free drug sensors (FDS) to measure free ionized drug concentrations in colloidal systems, including micellar solutions, emulsions, and lipid formulations during in vitro lipolysis. Diphenhydramine hydrochloride (DPH) and loperamide hydrochloride (LOP) were selected as model drugs. Self-diffusion nuclear magnetic resonance studies were performed and confirmed the entrapment of drugs in micelles in Brij 35 and sodium taurodeoxycholate (TDC)/phosphatidylcholine (PC) micellar solutions. The FDS measurements indicated that with a constant level of drug, the percentage of free DPH and LOP decreased from 84% to 57% and from 51% to 18%, respectively, as the concentration of Brij 35 was increased from 4.7 to 22 mM; and from 99% to 46% and from 100% to 21%, respectively, as the concentration of TDC/PC was increased from 0.49/0.04 to 8.85/0.78 mM. During the in vitro lipolysis of a lipid formulation, free drug concentration decreased with lipolysis time. The percentage of free DPH was higher than for LOP in the same colloidal system because DPH is less lipophilic than LOP. The study showed that FDS can be used to monitor the free drug concentration in colloidal systems with fast response, no sample treatment and simple data analysis.

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Formulation and characterization of self-nanoemulsifying drug delivery systems containing monoacyl phosphatidylcholine

Cited by 27 publications

References 27 publications

Self-Nanoemulsifying Drug Delivery System (SNEDDS) for Improved Oral Bioavailability of Chlorpromazine: In Vitro and In Vivo Evaluation

Self-Nanoemulsifying Drug Delivery System (SNEDDS) for Improved Oral Bioavailability of Chlorpromazine: In Vitro and In Vivo Evaluation

In Vitro Evaluation of Antimicrobial Activity and Cytotoxicity of Different Nanobiotics Targeting Multidrug Resistant and Biofilm Forming Staphylococci

Using Potentiometric Free Drug Sensors to Determine the Free Concentration of Ionizable Drugs in Colloidal Systems

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