Self-nanoemulsifying drug delivery system (SNEDDS) improves the oral bioavailability of betulinic acid

Bravo-Alfaro, Diego A.; Ochoa-Rodríguez, Laura R.; Villaseñor-Ortega, Francisco; Luna‐Bárcenas, Gabriel; Garcı́a, Hugo S.

doi:10.1016/j.molliq.2022.119946

Cited by 13 publications

(5 citation statements)

References 64 publications

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“…Moreover, they have found no changes in the particle size in the presence of simulated small intestinal phase conditions for 105 min. In vivo studies demonstrated about a 15-fold increment in the bioavailability of BA compared to free BA solution [54].…”

Section: Self-emulsifying Drug Delivery System (Sedds)mentioning

confidence: 99%

Lipid as a Vehicle/Carrier for Oral Drug Delivery

Desai¹,

Desai²,

Patel³

2023

Drug Formulation Design

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The drug administered by an oral route has to withstand a harsh environment of gastrointestinal media, absorb through intestinal epithelium and circumvent first-pass metabolism in liver before reaching portal blood circulation. Moreover, hydrophobic drug molecules offer challenges for formulation with respect to their solubility and hence bioavailability. Various approaches have been developed to overcome this barrier. One of them is the use of lipids in formulation. Incorporation of the drug in lipids can result in increased solubility, absorption and thereby enhanced bioavailability. Intestinal lymphatic route of absorption has also been explored for increasing bioavailability of hydrophobic drug moieties. In this chapter, we have discussed the pathway of lipid digestion in the human body as well as the mechanism of lipid particles upon oral administration. The various lipid formulations developed and the excipients used in the formulations have also been described. The importance of lipid chain length and the effect of food in increasing the bioavailability of drug is discussed. The lymphatic pathway of lipid carriers has also been discussed.

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Section: Self-emulsifying Drug Delivery System (Sedds)mentioning

confidence: 99%

Lipid as a Vehicle/Carrier for Oral Drug Delivery

Desai¹,

Desai²,

Patel³

2023

Drug Formulation Design

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“…Solubility studies were conducted using the method described by Bravo-Alfaro et al, in 2022 [11] with minor changes to determine the oil phase in which ETP can solubilize. To do this, various concentrations of ETP were put into Eppendorf tubes holding 1 mL of various oils, (sesame, ginger, castor, olive, geranium, sun ower, and coconut oils), surfactants (tween 80, tween 60, tween 40, tween 20) and cosurfactants (PEG 600, PEG 400 and PEG 200).…”

Section: Solubility Study Of Etp In Different Oils Surfactants and Co...mentioning

confidence: 99%

Antidepressant and Pharmacokinetic Evaluation of Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) of Escitalopram

Asaad,

Majeed,

Abbas

et al. 2023

Preprint

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Escitalopram (ETP) has poor oral bioavailability due to its low water solubility, hence the goal of this work was to design and optimize a self-nano-emulsifying drug delivery system (SNEDDS). Using the results of the investigations on solubility and emulsification, a pseudo-ternary phase diagram was produced. The three main ingredients chosen for the formulation were polyethylene glycol 400 (co-surfactant), tween 80 (surfactant), and geranium oil (lipid). ETP-SNEDDS was evaluated for the size of particles and surface charge. Fourier transforms infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) were used to evaluate the chemical compatibility and thermal stability. Ex-vivo permeability, in vitro digestion, and in vitro dissolution investigations were carried out and compared with reference tablets. The bioavailability of ETP-loaded SNEDDS was evaluated in comparison to the control in Wistar rats (n = 6). With a droplet size of 145 nm, a polydispersity index of 0.120, and an emulsification period of almost one minute, the synthesized SNEDDS were thermodynamically stable. The ETP-loaded SNEDDS displayed 96% dissolution in FSSIF. The permeation investigation revealed that, in comparison to the ETP powder and reference tablet, respectively, the SNEDDS increased drug penetration by 4.2 and 3.1-folds. The enhancement of in vitro dissolution, in vitro digestion, and ex-vivo permeability was found significant (p < 0.05). In comparison to the reference, SNEDDS had Cmax and AUC increases of 5.34 and 4.71 fold, respectively. These findings suggested that the SNEDDS formulation would be a promising method for increasing the oral bioavailability and absorption of ETP.

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“…To address the low bioavailability of BBEs, various approaches have been developed, including physical modification, chemical modification, and formulation strategies. Physical modification techniques, such as micronization [ 20 ], nanoemulsification [ 21 , 22 , 23 ], and solid dispersion [ 20 , 24 ], are used to increase the surface area and reduce the particle size of BBE. Chemical modifications, for example, esterification [ 25 , 26 , 27 ], glycosylation, acylation [ 10 , 17 , 28 ], and the synthesis of prodrugs, aim to improve the chemical stability and lipophilicity of BBEs [ 29 ].…”

Section: Introductionmentioning

confidence: 99%

Innovative Approach to Enhance Bioavailability of Birch Bark Extracts: Novel Method of Oleogel Development Contrasted with Other Dispersed Systems

Andze,

Vitolina,

Berzins

et al. 2024

Plants

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Birch outer bark extract (BBE), containing pentacyclic triterpenes such as betulin, lupeol, and betulinic acid, is a widely recognized natural product renowned for its diverse pharmacological effects. However, its limited water solubility restricts its bioavailability. Therefore, the main objective is to enhance the bioavailability of BBE for pharmaceutical use. In this study, we aimed to develop a dispersion system utilizing a unique oleogel-producing method through the recrystallization of BBE from an ethanol solution in the oil phase. We generated an oleogel that demonstrates a notable 42–80-fold improvement in betulin and lupeol peroral bioavailability from BBE in Wistar rats, respectively. A physical paste-like BBE hydrogel developed with antisolvent precipitation showed a 16–56-fold increase in the bioavailability of betulin and lupeol from BBE in rat blood plasma, respectively. We also observed that the repeated administration of the BBE oleogel did not exhibit any toxicity at the tested dose (38.5 mg/kg betulin, 5.2 mg/kg lupeol, 1.5 mg/kg betulinic acid daily for 7 days). Betulin and betulinic acid were not detected in rat heart, liver, kidney, or brain tissues after the peroral administration of the oleogel daily for 7 days. Lupeol was found in rat heart, liver, and kidney tissues.

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Self-nanoemulsifying drug delivery system (SNEDDS) improves the oral bioavailability of betulinic acid

Cited by 13 publications

References 64 publications

Lipid as a Vehicle/Carrier for Oral Drug Delivery

Lipid as a Vehicle/Carrier for Oral Drug Delivery

Antidepressant and Pharmacokinetic Evaluation of Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) of Escitalopram

Innovative Approach to Enhance Bioavailability of Birch Bark Extracts: Novel Method of Oleogel Development Contrasted with Other Dispersed Systems

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