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Preparation, characterization and release behavior of chitosan-coated nanoliposomes (chitosomes) containing olive leaf extract optimized by response surface methodology.

ABSTRACT: This study was dedicated to the optimization and preparation of chitosan-coated liposomes (chitosomes) as promising nanocarriers for retention of olive leaf extract optimized by Response surface methodology (RSM) based on central composite design. Accordingly, the best sample was chosen for further tests with the encapsulation efficiency, stability and electrical conductivity of 94%, 98% and 9.545 mS respectively. The average size of the optimal chitosome and nanoliposome were lower than 100 nm and the zeta potential was altered from a negative charge to positive after addition coating process with chitosan. Moreover, the differential scanning calorimetry of blank and loaded chitosome revealed the increase of fluidity and lower temperature of phase transition in loaded chitosome compared to blank one. FTIR spectra demonstrated that electrostatic interactions and hydrogen bonds occur between phospholipid polar groups, chitosan amine moieties and major olive leaf extract polyphenols including oleuropein and hydroxy tyrosol. Furthermore, the optimal loaded chitosome had the highest stability during 25 days at the temperature of 4 °C. Finally, the in vitro release tests were best fitted with Peppas-Sahlin and Kopcha models in food simulants and gastrointestinal simulated juice respectively revealing erosion-based release model.

Supplementary information

The online version contains supplementary material available at (10.1007/s13197-021-04972-2).

SUBMITTER: Katouzian I

PROVIDER: S-EPMC8292535 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature

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Preparation, characterization and release behavior of chitosan-coated nanoliposomes (chitosomes) containing olive leaf extract optimized by response surface methodology.

Katouzian Iman I Taheri Ramezan Ali RA

Journal of food science and technology 20210125 9

This study was dedicated to the optimization and preparation of chitosan-coated liposomes (chitosomes) as promising nanocarriers for retention of olive leaf extract optimized by Response surface methodology (RSM) based on central composite design. Accordingly, the best sample was chosen for further tests with the encapsulation efficiency, stability and electrical conductivity of 94%, 98% and 9.545 mS respectively. The average size of the optimal chitosome and nanoliposome were lower than 100 nm ...[more]

PMID: 34366460

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Project description:A key diterpene lactone of Andrographis paniculata, i.e., andrographolide (AG), exhibits a variety of physiological properties, including hepatoprotection. The limited solubility, short half-life, and poor bioavailability limits the pharmacotherapeutic potential of AG. Therefore, in this study we aimed to formulate and optimize AG-loaded nanoliposomes (AGL) using the Design of Experiment (DOE) approach and further modify the surface of the liposomes with mannosylated chitosan to enhance its oral bioavailability. Physical, morphological, and solid-state characterization was performed to confirm the formation of AGL and Mannosylated chitosan-coated AGL (MCS-AGL). Molecular docking studies were conducted to understand the ligand (MCS) protein (1EGG) type of interaction. Further, in vitro release, ex vivo drug permeation, and in vivo pharmacokinetics studies were conducted. The morphological studies confirmed that AGL was spherical and a layer of MCS coating was observed on their surface, forming the MCS-AGL. Further increase in the particle size and change in the zeta potential of MCS-AGL confirms the coating on the surface of AGL (375.3 nm, 29.80 mV). The in vitro drug release data reflected a sustained drug release profile from MCS-AGL in the phosphate buffer (pH 7.4) with 89.9 ± 2.13% drug release in 8 h. Ex vivo permeation studies showed higher permeation of AG from MCS-AGL (1.78-fold) compared to plain AG and AGL (1.37-fold), indicating improved permeability profiles of MCS-AGL. In vivo pharmacokinetic studies inferred that MCS-AGL had a 1.56-fold enhancement in AUC values compared to plain AG, confirming that MCS-AGL improved the bioavailability of AG. Additionally, the 2.25-fold enhancement in the MRT proves that MCS coating also enhances the in vivo stability and retention of AG (stealth effect). MCS as a polymer therefore has a considerable potential for improving the intestinal permeability and bioavailability of poorly soluble and permeable drugs or phytoconstituents when coated over nanocarriers.

Dataset Information

Preparation, characterization and release behavior of chitosan-coated nanoliposomes (chitosomes) containing olive leaf extract optimized by response surface methodology.

Supplementary information

Publications

Preparation, characterization and release behavior of chitosan-coated nanoliposomes (chitosomes) containing olive leaf extract optimized by response surface methodology.

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