Influence of the Encapsulation Efficiency and Size of Liposome on the Oral Bioavailability of Griseofulvin-Loaded Liposomes

Ong, Sandy Gim Ming; Ming, Long Chiau; Lee, Kah Seng; Yuen, Kah Hay

doi:10.3390/pharmaceutics8030025

Cited by 160 publications

(83 citation statements)

References 63 publications

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“…Therefore, sonication is also not the method of choice for size reduction. In FTS method, the freezing and thawing process was aimed at producing physical disruption to the liposomal phospholipid bilayers [27,35] while the sonication process was intended to reduce the size of liposomes [36]. The present findings suggest that the capacity of the FTS method is comparable to that of the extrusion method in reducing the size of liposomes.…”

Section: Discussionmentioning

confidence: 68%

Evaluation of Extrusion Technique for Nanosizing Liposomes

et al. 2016

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The aim of the present study was to study the efficiency of different techniques used for nanosizing liposomes. Further, the aim was also to evaluate the effect of process parameters of extrusion techniques used for nanosizing liposomes on the size and size distribution of the resultant liposomes. To compare the efficiency of different nanosizing techniques, the following techniques were used to nanosize the liposomes: extrusion, ultrasonication, freeze-thaw sonication (FTS), sonication and homogenization. The extrusion technique was found to be the most efficient, followed by FTS, ultrasonication, sonication and homogenization. The extruder used in the present study was fabricated using readily available and relatively inexpensive apparatus. Process parameters were varied in extrusion technique to study their effect on the size and size distribution of extruded liposomes. The results obtained indicated that increase in the flow rate of the extrusion process decreased the size of extruded liposomes however the size homogeneity was negatively impacted. Furthermore, the liposome size and distribution was found to decline with decreasing membrane pore size. It was found that by extruding through a filter with a pore size of 0.2 µm and above, the liposomes produced were smaller than the pore size, whereas, when they were extruded through a filter with a pore size of less than 0.2 µm the resultant liposomes were slightly bigger than the nominal pore size. Besides that, increment of extrusion temperature above transition temperature of the pro-liposome had no effect on the size and size distribution of the extruded liposomes. In conclusion, the extrusion technique was reproducible and effective among all the methods evaluated. Furthermore, processing parameters used in extrusion technique would affect the size and size distribution of liposomes. Therefore, the process parameters need to be optimized to obtain a desirable size range and homogeneity, reproducible for various in vivo applications.

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Section: Discussionmentioning

confidence: 68%

Evaluation of Extrusion Technique for Nanosizing Liposomes

et al. 2016

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“…To determine drug encapsulation efficiency, nanoemulsion formulation samples (1 mL) were added to Eppendorf centrifuge tubes, then subjected to ultracentrifugation (Beckman Optima L-80, Beckman, Brea, CA, USA) at 13,000 × g for 2 hrs to obtain a clear supernatant. 21 The supernatant solution (0.1 mL) was withdrawn and stored at 4°C until analysis. The supernatant was diluted with a 1:1 (v/v, 2.9 mL) methanol:water mixture to determine RIF content, and %EE was calculated using the following equation 3:…”

Section: Percent Encapsulation Efficiency Studymentioning

confidence: 99%

<p>Novel Approach for Transdermal Delivery of Rifampicin to Induce Synergistic Antimycobacterial Effects Against Cutaneous and Systemic Tuberculosis Using a Cationic Nanoemulsion Gel</p>

Hussain¹,

Altamimi²,

Alshehri³

et al. 2020

IJN

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This study demonstrated improved transdermal delivery of rifampicin-loaded cationic nanoemulsion gel to treat systemic and cutaneous tuberculosis using capmul, labrasol, and acconon, which exert anti-Mycobacterium activities. This approach enhanced drug permeation across the skin, increased therapeutic efficacy, and reduced dose-related side effects. Methods: Design Expert ® was used to optimize formulations (S mix ratio and capmul as independent factors), which were prepared using a slow spontaneous titration method. The optimized nanoemulsion was incorporated into carbopol gel to allow for topical application and comparative assessments. Nanoemulsions and gels were evaluated for size, size distribution, shape, zeta potential, percent spread, viscosity, in vitro hemolysis, in vitro release, and ex vivo skin permeation and deposition. A mechanistic evaluation was performed using scanning electron microscopy. Furthermore, in vivo pharmacokinetic and irritation studies were performed. Results: The optimized cationic nanoemulsion (OCNE-1) was characterized by small particle size (≤100 nm), had optimal viscosity, percent spread, zeta potential, and percent drug release, and was hemocompatible. The OCNE-1T gel exhibited higher permeation flux (51.32 ± 0.5 µg/cm 2 hr), permeation coefficient (2.566 ± 0.08 cm/hr), drug deposition (994.404 µg/cm 2), and enhancement ratio (7.16) than those of the OCNE-1 nanoemulsion or drug solution. Scanning electron microscopy was used to characterize the mechanism of enhanced permeation. An In vivo study showed that the C max and area under the curve following transdermal application were 4.34-and 4.74-fold higher than those following oral administration. Conclusion: Transdermal delivery of rifampicin could be a promising alternative to conventional approaches to treat systemic and local tuberculosis, and other bacterial infections.

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“…Freshly prepared NHNK samples were centrifuged to separate different fractions of honokiol, following with the protocol described in the previous study. 36 Each fraction was redissolved in methanol and analyzed using HPLC. The amount of honokiol in each fraction was estimated based on corresponding concentrations from the absorption response in the calibration curve, and the encapsulation efficiency was estimated to be 58.1 ± 4.2%.…”

Section: Determination Of Encapsulation Efficiency Of Nhnkmentioning

confidence: 99%

<p>Development of Nanosome-Encapsulated Honokiol for Intravenous Therapy Against Experimental Autoimmune Encephalomyelitis</p>

Hsiao¹,

Chen²,

Liang³

et al. 2020

IJN

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Background: Honokiol has been reported to possess anti-inflammatory and neuroprotective activities. However, the poor aqueous solubility of honokiol limits its clinical application for systemic administration. Purpose: This study aims to develop a novel formulation of nanosome-encapsulated honokiol (NHNK) for intravenous therapy against mouse experimental autoimmune encephalomyelitis (EAE) that mimics human multiple sclerosis. Methods: Nanosomes and NHNK were prepared by using an ultra-high pressure homogenization (UHPH) method. Mice were treated with NHNK or empty nanosomes during the peak phase of EAE symptoms. Symptoms of EAE were monitored and samples of the spinal cord were obtained for histopathological examinations. Results: The stock of NHNK containing honokiol in the nanosome formulation, which showed the structure of single phospholipid bilayer membranes, was well formulated with the particle size of 48.0 ± 0.1 nm and the encapsulation efficiency 58.1 ± 4.2%. Intravenous administration of NHNK ameliorated the severity of EAE accompanied by a significant reduction of demyelination and inflammation in the spinal cord. Furthermore, NHNK decreased the number of IL-6 + , Iba-1 + TNF + , Iba-1 + IL-12 p40 + , and CD3 + IFN-γ + cells infiltrating the spinal cord. Conclusion: The UHPH method simplified the preparation of NHNK with uniformly distributed nanosize and high encapsulation efficiency. Intravenous administration of NHNK ameliorated the severity of EAE by suppressing the infiltration of activated microglia and Th1 cells into the spinal cord. Collectively, these results suggest that the formulation of NHNK is a prospective therapeutic approach for inflammatory CNS diseases, such as multiple sclerosis.

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Influence of the Encapsulation Efficiency and Size of Liposome on the Oral Bioavailability of Griseofulvin-Loaded Liposomes

Cited by 160 publications

References 63 publications

Evaluation of Extrusion Technique for Nanosizing Liposomes

Evaluation of Extrusion Technique for Nanosizing Liposomes

<p>Novel Approach for Transdermal Delivery of Rifampicin to Induce Synergistic Antimycobacterial Effects Against Cutaneous and Systemic Tuberculosis Using a Cationic Nanoemulsion Gel</p>

<p>Development of Nanosome-Encapsulated Honokiol for Intravenous Therapy Against Experimental Autoimmune Encephalomyelitis</p>

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