Formulation, characterization and in-vitro evaluation of self-nanoemulsifying drug delivery system containing rhamnolipid biosurfactant

Research output: Contribution to journalJournal articlepeer-review

Standard

Formulation, characterization and in-vitro evaluation of self-nanoemulsifying drug delivery system containing rhamnolipid biosurfactant. / Khan, Muhammad Ahsan; Ullah, Kaleem; Rahman, Nisar ur; Mahmood, Arshad; Müllertz, Anette; Mannan, Abdul; Murtaza, Ghulam; Khan, Shujaat Ali.

In: Journal of Drug Delivery Science and Technology, Vol. 75, 103673, 2022.

Research output: Contribution to journalJournal articlepeer-review

Harvard

Khan, MA, Ullah, K, Rahman, NU, Mahmood, A, Müllertz, A, Mannan, A, Murtaza, G & Khan, SA 2022, 'Formulation, characterization and in-vitro evaluation of self-nanoemulsifying drug delivery system containing rhamnolipid biosurfactant', Journal of Drug Delivery Science and Technology, vol. 75, 103673. https://doi.org/10.1016/j.jddst.2022.103673

APA

Khan, M. A., Ullah, K., Rahman, N. U., Mahmood, A., Müllertz, A., Mannan, A., Murtaza, G., & Khan, S. A. (2022). Formulation, characterization and in-vitro evaluation of self-nanoemulsifying drug delivery system containing rhamnolipid biosurfactant. Journal of Drug Delivery Science and Technology, 75, [103673]. https://doi.org/10.1016/j.jddst.2022.103673

Vancouver

Khan MA, Ullah K, Rahman NU, Mahmood A, Müllertz A, Mannan A et al. Formulation, characterization and in-vitro evaluation of self-nanoemulsifying drug delivery system containing rhamnolipid biosurfactant. Journal of Drug Delivery Science and Technology. 2022;75. 103673. https://doi.org/10.1016/j.jddst.2022.103673

Author

Khan, Muhammad Ahsan ; Ullah, Kaleem ; Rahman, Nisar ur ; Mahmood, Arshad ; Müllertz, Anette ; Mannan, Abdul ; Murtaza, Ghulam ; Khan, Shujaat Ali. / Formulation, characterization and in-vitro evaluation of self-nanoemulsifying drug delivery system containing rhamnolipid biosurfactant. In: Journal of Drug Delivery Science and Technology. 2022 ; Vol. 75.

Bibtex

@article{e7a0370e79534721be530993fd036e52,
title = "Formulation, characterization and in-vitro evaluation of self-nanoemulsifying drug delivery system containing rhamnolipid biosurfactant",
abstract = "Self-nanoemulsifying drug delivery systems (SNEDDS) are most commonly used lipid-based drug delivery systems for bioavailability enhancement. Mostly SNEDDS contains high concentrations of synthetic surfactants which may result in gastric irritation and cause toxicity. In this study, Rhamnolipid, a biosurfactant, is utilized as a cosurfactant to minimize the quantity of synthetic surfactant in SNEDDS formulation. Two sets of SNEDDS formulations comprising of medium-chain (MC) or long-chain (LC) glycerides, Kolliphor {\textregistered} RH40 (KOL) and Rhamnolipid (RL) were produced using a D-optimal design in MODDE software. The monodispersed SNEDDS preconcentrates were further characterized by utilizing dynamic light scattering (at pH 2.5 & 6.5), cryogenic transmission electron microscopy, thermodynamic stability, in-vitro lipid digestion, and viscosity measurements. All MC-SNEDDS preconcentrates were not homogenous and considered unstable, while LC-SNEDDS were homogenous and produced nanoemulsions with droplet sizes ranging from 21 to 336 nm. LC-SNEDDS formulations containing RL produced smaller droplet sizes when dispersed in simulated intestinal media while droplet size slightly increased in the simulated gastric fluid which suggested that RL reduces droplet size more efficiently at higher pH. The zeta potential of nanoemulsion produced by dispersion of LC-SNEDDS containing RL was decreased at low pH. Thermodynamic stability studies have shown that all selected preconcentrates were stable. During in vitro lipolysis, only 24–34% of formulations were enzymatically digested, and at higher concentrations of RL, low number of fatty acids was released. Based on the results of dynamic viscosity studies, all the formulations showed non-Newtonian properties and were suitable for the capsule filling process. During cytotoxicity studies, LC-SNEDDS formulation and RL cosurfactant were well-tolerable at doses normally administered to human. In conclusion, this study demonstrated that LC-SNEDDS comprising RL as cosurfactant are favorable formulations when reduction in the amount of synthetic surfactant is desirable and RL also possibly helps to alter the digestion rate.",
keywords = "Cryogenic transmission electron microscopy, Cytotoxicity study, Design of experiment, In-vitro lipolysis, Rhamnolipid, Self-nanoemulsifying drug delivery system",
author = "Khan, {Muhammad Ahsan} and Kaleem Ullah and Rahman, {Nisar ur} and Arshad Mahmood and Anette M{\"u}llertz and Abdul Mannan and Ghulam Murtaza and Khan, {Shujaat Ali}",
note = "Publisher Copyright: {\textcopyright} 2022 Elsevier B.V.",
year = "2022",
doi = "10.1016/j.jddst.2022.103673",
language = "English",
volume = "75",
journal = "Journal of Drug Delivery Science and Technology",
issn = "1773-2247",
publisher = "Elsevier",

}

RIS

TY - JOUR

T1 - Formulation, characterization and in-vitro evaluation of self-nanoemulsifying drug delivery system containing rhamnolipid biosurfactant

AU - Khan, Muhammad Ahsan

AU - Ullah, Kaleem

AU - Rahman, Nisar ur

AU - Mahmood, Arshad

AU - Müllertz, Anette

AU - Mannan, Abdul

AU - Murtaza, Ghulam

AU - Khan, Shujaat Ali

N1 - Publisher Copyright: © 2022 Elsevier B.V.

PY - 2022

Y1 - 2022

N2 - Self-nanoemulsifying drug delivery systems (SNEDDS) are most commonly used lipid-based drug delivery systems for bioavailability enhancement. Mostly SNEDDS contains high concentrations of synthetic surfactants which may result in gastric irritation and cause toxicity. In this study, Rhamnolipid, a biosurfactant, is utilized as a cosurfactant to minimize the quantity of synthetic surfactant in SNEDDS formulation. Two sets of SNEDDS formulations comprising of medium-chain (MC) or long-chain (LC) glycerides, Kolliphor ® RH40 (KOL) and Rhamnolipid (RL) were produced using a D-optimal design in MODDE software. The monodispersed SNEDDS preconcentrates were further characterized by utilizing dynamic light scattering (at pH 2.5 & 6.5), cryogenic transmission electron microscopy, thermodynamic stability, in-vitro lipid digestion, and viscosity measurements. All MC-SNEDDS preconcentrates were not homogenous and considered unstable, while LC-SNEDDS were homogenous and produced nanoemulsions with droplet sizes ranging from 21 to 336 nm. LC-SNEDDS formulations containing RL produced smaller droplet sizes when dispersed in simulated intestinal media while droplet size slightly increased in the simulated gastric fluid which suggested that RL reduces droplet size more efficiently at higher pH. The zeta potential of nanoemulsion produced by dispersion of LC-SNEDDS containing RL was decreased at low pH. Thermodynamic stability studies have shown that all selected preconcentrates were stable. During in vitro lipolysis, only 24–34% of formulations were enzymatically digested, and at higher concentrations of RL, low number of fatty acids was released. Based on the results of dynamic viscosity studies, all the formulations showed non-Newtonian properties and were suitable for the capsule filling process. During cytotoxicity studies, LC-SNEDDS formulation and RL cosurfactant were well-tolerable at doses normally administered to human. In conclusion, this study demonstrated that LC-SNEDDS comprising RL as cosurfactant are favorable formulations when reduction in the amount of synthetic surfactant is desirable and RL also possibly helps to alter the digestion rate.

AB - Self-nanoemulsifying drug delivery systems (SNEDDS) are most commonly used lipid-based drug delivery systems for bioavailability enhancement. Mostly SNEDDS contains high concentrations of synthetic surfactants which may result in gastric irritation and cause toxicity. In this study, Rhamnolipid, a biosurfactant, is utilized as a cosurfactant to minimize the quantity of synthetic surfactant in SNEDDS formulation. Two sets of SNEDDS formulations comprising of medium-chain (MC) or long-chain (LC) glycerides, Kolliphor ® RH40 (KOL) and Rhamnolipid (RL) were produced using a D-optimal design in MODDE software. The monodispersed SNEDDS preconcentrates were further characterized by utilizing dynamic light scattering (at pH 2.5 & 6.5), cryogenic transmission electron microscopy, thermodynamic stability, in-vitro lipid digestion, and viscosity measurements. All MC-SNEDDS preconcentrates were not homogenous and considered unstable, while LC-SNEDDS were homogenous and produced nanoemulsions with droplet sizes ranging from 21 to 336 nm. LC-SNEDDS formulations containing RL produced smaller droplet sizes when dispersed in simulated intestinal media while droplet size slightly increased in the simulated gastric fluid which suggested that RL reduces droplet size more efficiently at higher pH. The zeta potential of nanoemulsion produced by dispersion of LC-SNEDDS containing RL was decreased at low pH. Thermodynamic stability studies have shown that all selected preconcentrates were stable. During in vitro lipolysis, only 24–34% of formulations were enzymatically digested, and at higher concentrations of RL, low number of fatty acids was released. Based on the results of dynamic viscosity studies, all the formulations showed non-Newtonian properties and were suitable for the capsule filling process. During cytotoxicity studies, LC-SNEDDS formulation and RL cosurfactant were well-tolerable at doses normally administered to human. In conclusion, this study demonstrated that LC-SNEDDS comprising RL as cosurfactant are favorable formulations when reduction in the amount of synthetic surfactant is desirable and RL also possibly helps to alter the digestion rate.

KW - Cryogenic transmission electron microscopy

KW - Cytotoxicity study

KW - Design of experiment

KW - In-vitro lipolysis

KW - Rhamnolipid

KW - Self-nanoemulsifying drug delivery system

U2 - 10.1016/j.jddst.2022.103673

DO - 10.1016/j.jddst.2022.103673

M3 - Journal article

AN - SCOPUS:85135947315

VL - 75

JO - Journal of Drug Delivery Science and Technology

JF - Journal of Drug Delivery Science and Technology

SN - 1773-2247

M1 - 103673

ER -

ID: 318195408