Development and Percutaneous Permeation Study of Escinosomes, Escin-Based Nanovesicles Loaded with Berberine Chloride

Escin is a natural saponin, clinically used for the anti-edematous and anti-inflammatory effects. The aim of the study was to explore the possibility of converting escin into vesicle bilayer-forming component. The hyaluronidase inhibition activity of escin was evaluated after its formulation in escinosomes. Berberine chloride, a natural quaternary isoquinoline alkaloid isolated from several medicinal plants that is traditionally used for various skin conditions was loaded in the vesicles. The developed nanovesicles were characterized in terms of diameter, polydispersity, ζ-potential, deformability, recovery, encapsulation efficiency, stability, and release kinetics. Nanovesicle permeation properties through artificial membranes and rabbit ear skin were investigated using skin-PAMPATM and Franz cells were also evaluated. Escinosomes, made of phosphatidylcholine and escin, were loaded with berberine chloride. These nanovesicles displayed the best characteristics for skin application, particularly optimal polydispersity (0.17) and deformability, high negative ζ-potential value, great encapsulation efficiency (about 67%), high stability, and the best release properties of berberine chloride (about 75% after 24 h). In conclusion, escinosomes seem to be new vesicular carriers, capable to maintain escin properties such as hyaluronidase inhibition activity, and able to load other active molecules such as berberine chloride, in order to enhance or expand the activity of the loaded drug.

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Programmable Release of Berberine Chloride Hydrate from Shape Memory Fibers Prepared from Core-Sheath Wet-Spinning Technology

Journal of Biomedical Nanotechnology ◽

10.1166/jbn.2019.2784 ◽

2019 ◽

Vol 15 (7) ◽

pp. 1432-1442 ◽

Cited By ~ 7

Author(s):

Jiamin Tang ◽

Ruifang Zhao ◽

Xueqian Yin ◽

Ya Wen ◽

Yidong Shi ◽

...

Keyword(s):

Shape Memory ◽

Release Kinetics ◽

Drug Carrier ◽

Wet Spinning ◽

Therapeutic Drug ◽

Composite Fibers ◽

Practical Applications ◽

Berberine Chloride ◽

Chloride Hydrate

Smart wet-spun fibers for highly programmable release of therapeutic drug have been rarely reported. Herein, thermalresponsive composite fibers were successfully prepared by core-sheath wet-spinning technology in present study. They consisted of a model drug of natural antibacterial berberine chloride hydrate (BCH) and a drug carrier of temperature responsive shape memory polyurethane (SMPU). The obtained composite fibers featured with well-controlled microscopic morphologies, exhibiting significantly enhanced thermal stability and superb mechanical properties. In vitro drug release test and corresponding release kinetics study were performed for investigation of BCH's release behavior. Results demonstrated that the release behaviors of BCH from the core-sheath fibers were pH-dependent, influenced by both diffusion from pore channels and the solubility of BCH in the release mediums, and BCH imbedded only in core part showed a longer release period compared with that in both core and sheath parts of the composite fibers. More importantly, the release rate of BCH can be simply controlled by changing the initial shapes of fibers through stretching and fixation of the stretched deformations. Furthermore, the antibacterial durability of the smart composites fibers was demonstrated and tracked according to the growth inhibition against both negative E. coli and positive S. aureus bacteria strains. All these results suggest that the developed composite fibers can be promising candidates as smart drug delivery vehicles for highly adjustable doses of target drugs towards practical applications.

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Encapsulation efficiency and release kinetics of solid and liquid pesticides through urea formaldehyde crosslinked starch, guar gum, and starch + guar gum matrices

Journal of Applied Polymer Science ◽

10.1002/app.2141 ◽

2001 ◽

Vol 82 (11) ◽

pp. 2863-2866 ◽

Cited By ~ 34

Author(s):

Sangamesh G. Kumbar ◽

Anandrao R. Kulkarni ◽

Ashok M. Dave ◽

Tejraj M. Aminabhavi

Keyword(s):

Encapsulation Efficiency ◽

Guar Gum ◽

Release Kinetics ◽

Urea Formaldehyde ◽

Kinetics Of

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Organically modified silica nanoparticles as drug delivery vehicles in photodynamic therapy

Journal of Porphyrins and Phthalocyanines ◽

10.1142/s1088424611003306 ◽

2011 ◽

Vol 15 (05n06) ◽

pp. 401-411 ◽

Cited By ~ 6

Author(s):

Anurag Gupta ◽

Lalit N. Goswami ◽

Manivannan Ethirajan ◽

Joseph Missert ◽

K.V.R. Rao ◽

...

Keyword(s):

Silica Nanoparticles ◽

Encapsulation Efficiency ◽

Release Kinetics ◽

Alkyl Ether ◽

Modified Silica ◽

Drug Delivery Vehicles ◽

Organically Modified ◽

Delivery Vehicles ◽

Organically Modified Silica ◽

Modified Silica Nanoparticles

To investigate the effect of hydrophobicity, charge and size of photosensitizers (PS) on their encapsulation efficiency in organically modified silica nanoparticles (ORMOSIL), a series of alkyl ether analogs of 2-(1′-hexyloxyethyl)-2-devinyl pyropheophorbide-a (HPPH) containing varied number of carbon units, HPPH with anionic and cationic functionalities, and HPPH analogs with molecular weight ranging from ~630 to 6000 Daltons were synthesized. Our preliminary results suggest that these factors play a significant role in encapsulation of the photosensitizers and their release from ORMOSIL nanoparticles. The synthesis and characterization of PS-encapsulated ORMOSIL and a comparative study on the effect of PS size, lipophilicity and charge on encapsulation efficiency, photophysical characteristics and release kinetics are discussed.

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Liposomes as Vancomycin Hydrochloride Delivery System

Key Engineering Materials ◽

10.4028/www.scientific.net/kem.903.3 ◽

2021 ◽

Vol 903 ◽

pp. 3-8

Author(s):

Mārīte Skrinda ◽

Arita Dubnika ◽

Janis Locs

Keyword(s):

Drug Delivery ◽

Drug Administration ◽

Delivery System ◽

Drug Delivery Systems ◽

Encapsulation Efficiency ◽

Release Kinetics ◽

Delivery Systems ◽

Free Drug ◽

Hydrophobic Drugs ◽

Vancomycin Hydrochloride

Liposomes are being used as unique drug delivery systems due to their ability to encapsulate both hydrophilic and hydrophobic drugs, as well as for the fact that they improve the disadvantages of free drug administration. However, liposomes have a significant disadvantage - low encapsulation efficiency. In the research carried out, 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) and cholesterol (Chol), in the ratio (n/n) of 2:1, 3:1 and 4:1 respectively, were used to prepare the liposomes. Blank liposomes (LIP) and vancomycin hydrochloride (VANKA) containing liposomes (VANKA-LIP) were prepared for each of the DSPC and Chol compositions. The aim of our study was to evaluate the effect of liposome composition on the VANKA encapsulation efficiency and release kinetics.

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Glycyrrhetinic Acid Liposomes and Hyalurosomes on Spanish Broom, Flax, and Hemp Dressings to Heal Skin Wounds

Molecules ◽

10.3390/molecules25112558 ◽

2020 ◽

Vol 25 (11) ◽

pp. 2558 ◽

Cited By ~ 2

Author(s):

Angela Abruzzo ◽

Concettina Cappadone ◽

Giovanna Farruggia ◽

Barbara Luppi ◽

Federica Bigucci ◽

...

Keyword(s):

Size Distribution ◽

Encapsulation Efficiency ◽

Healing Process ◽

In Vitro Release ◽

Glycyrrhetinic Acid ◽

Skin Wounds ◽

Ζ Potential ◽

Biological Studies ◽

Vitro Release

The focus of this work was to prepare Spanish Broom, flax, and hemp dressings impregnated with glycyrrhetinic acid (GA) liposomes or hyalurosomes to promote the healing process and protect the skin wounds. Vesicles were prepared by the film hydration method and characterized in terms of size, particle size distribution, ζ potential, encapsulation efficiency, in vitro release, and biocompatibility on 3T3 fibroblasts. Loaded liposomes and hyalurosomes showed nanometric size (355 ± 19 nm and 424 ± 32 nm, respectively), good size distribution (lower than 0.3), and appropriate encapsulation efficiency (58.62 ± 3.25% and 59.22 ± 8.18%, respectively). Hyalurosomes showed good stability during the storage period, which can be correlated to the negative ζ potential, and allowed a fast and complete release of GA. Preliminary biological studies revealed that both kinds of loaded vesicles were not cytotoxic and that hyalurosomes could exert a slight stimulating effect on fibroblast proliferation. Finally, in vitro release studies from the different dressings impregnated with the loaded vesicles demonstrated that a high amount of GA could be reached at the wound site after 60 min from application. In conclusion, the results suggested that the developed dressings, especially those impregnated with hyalurosomes, can be efficiently used to promote the healing process.

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Co-Delivery of Berberine Chloride and Tariquidar in Nanoliposomes Enhanced Intracellular Berberine Chloride in a Doxorubicin-Resistant K562 Cell Line Due to P-gp Overexpression

Pharmaceutics ◽

10.3390/pharmaceutics13030306 ◽

2021 ◽

Vol 13 (3) ◽

pp. 306 ◽

Cited By ~ 1

Author(s):

Giulia Vanti ◽

Marcella Coronnello ◽

Daniele Bani ◽

Antonella Mannini ◽

Maria Camilla Bergonzi ◽

...

Keyword(s):

Horseradish Peroxidase ◽

Cell Line ◽

Tumor Cells ◽

Cell Lines ◽

K562 Cell ◽

Encapsulation Efficiency ◽

Antitumor Agent ◽

K562 Cell Line ◽

Berberine Chloride ◽

Chloride Accumulation

The MDR phenomenon has become a major obstacle in the treatment of cancers, and among the strategies to reverse it, the inhibition of P-gp function and expression is essential to increase for effective anticancer drugs. In the present paper, the co-delivery of berberine chloride and tariquidar loaded nanoliposomes was investigated with the aim of enhancing solubility and improving desired effects for the antineoplastic drug and the P-gp inhibitor. Developed nanoliposomes were loaded with the electron-dense enzyme horseradish peroxidase, and analyzed by TEM to investigate their ability to enter in both K562 and K562/DOXO cell lines. Receptor-mediated endocytosis was evidenced for both cell lines. Nanoliposomes were loaded with tariquidar, berberine chloride, or both, maintaining chemical and physical characteristics—i.e., size, homogeneity, and encapsulation efficiency—and high suitability for parenteral administration. Tariquidar was able to reverse the MDR in the K562/DOXO cell line. Tariquidar- and berberine chloride-loaded nanoliposomes showed a significant increase of berberine chloride accumulation in tumor cells, which could be correlated with resensitization of the resistant cells to the antitumor agent. These results suggest that the co-delivery of the P-gp inhibitor, tariquidar, and the cytotoxicity inducer, berberine chloride, looks like a promising approach to overcome the MDR.

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Development of Nicotinic Acid Controlled Release Tablets with Natural Phenolic Anti-oxidant Polymer by Encapsulation Technique

Journal of Natural Remedies ◽

10.18311/jnr/2020/25514 ◽

2021 ◽

Vol 20 (4) ◽

pp. 204

Author(s):

Ravi Manne ◽

Agilandeswari Devarajan

Keyword(s):

Drug Release ◽

Nicotinic Acid ◽

Encapsulation Efficiency ◽

Release Kinetics ◽

Diffusion Mechanism ◽

Fickian Diffusion ◽

Wet Granulation ◽

Stability Studies ◽

Cholesterol Lowering ◽

Drug Content

Nicotinic Acid (NA) is a cholesterol lowering agent used to treat dyslipidemia. Proanthocyanidins (PC) was selected as a drug and encapsulation material in which the later has a dual property of being a polymer as well as cholesterol lowering agent. The encapsulation of NA with different concentrations of (PC) was carried out by solvent evaporation technique. The encapsulated NA was converted to granules which were then compressed into tablets by wet granulation method. It was subjected to many pre-compression parameters evaluation such as flow properties, drug content and encapsulation efficiency. The tablets were evaluated for thickness, hardness, friability, <em>in vitro</em> release studies, release kinetics and stability studies. The evaluated parameters of the formulations showed compliance with pharmacopoeial standards. The encapsulation efficiency was 99.73% and 99.52% of drug content. The FT-IR spectrum did not show interaction between drug and polymer. The drug release in pH 1.2 was lesser than in pH 6.8 buffer. The encapsulated product released drug in controlled manner in alkaline medium. The drug release was 97.1% and release was extended up to 12 hrs. The optimized batch underwent stability studies as per ICH guidelines. It can be concluded that among all the formulations the F5 can be considered as optimized formulation. The optimized formulations showed non-fickian diffusion mechanism of release.

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Encapsulation of a Small Hydrophilic Drug in Injectable PLGA Microparticles for Treatment of Pancreatic Cancer

Inquiry@Queen's Undergraduate Research Conference Proceedings ◽

10.24908/iqurcp.9183 ◽

2018 ◽

Author(s):

Christina Schweitzer

Keyword(s):

Pancreatic Cancer ◽

Encapsulation Efficiency ◽

Dosage Form ◽

Tumour Growth ◽

Release Kinetics ◽

Double Emulsion ◽

Emulsion Method ◽

Hydrophilic Drug ◽

Neu1 Sialidase

Pancreatic cancer is the fourth largest cause of cancer-related deaths in Canada, and has the highest mortality rate of all major cancers. The typical methods of treatment: chemotherapy and radiation have significant side effects, as they do not target the tumour specifically. Targeted therapies are being developed that would specifically affect the pancreatic tumour, leaving healthy cells undamaged. A small, hydrophilic drug has been shown to inhibit the activity of Neu1 sialidase, an enzyme involved in the activation of the growth process, which is upregulated in tumour cells. Previous research has shown that encapsulation of the drug in a surgically implanted PLGA capsule allows for drug release over a period of several weeks, inhibiting tumour growth. A microparticle form is desired, to decrease the invasiveness of the treatment. Encapsulation of the drug was performed using an aqueous double-emulsion method, resulting in a drug encapsulation efficiency of 37%. A mean particle size of 125 was obtained, within the range acceptable for injectable particles. Further experiments will be performed to compare the encapsulation efficiency with microparticles prepared using an organic single-emulsion method. The release kinetics of the drug will be characterized in vitro using HPLC analysis, and its effectiveness in inhibiting tumour growth will be assessed using tumour cell cultures and animal models. Should this dosage form prove effective at inhibiting tumour growth, it may lead to the formulation of an injectable dosage form capable of sustained release.

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Halloysite Nanotubes Coated by Chitosan for the Controlled Release of Khellin

Polymers ◽

10.3390/polym12081766 ◽

2020 ◽

Vol 12 (8) ◽

pp. 1766 ◽

Cited By ~ 3

Author(s):

Lorenzo Lisuzzo ◽

Giuseppe Cavallaro ◽

Stefana Milioto ◽

Giuseppe Lazzara

Keyword(s):

Contact Angle ◽

Controlled Release ◽

Water Contact Angle ◽

Electrostatic Interactions ◽

Release Kinetics ◽

Halloysite Nanotubes ◽

Hybrid Nanostructures ◽

Water Contact ◽

Ζ Potential ◽

Novel Strategy

In this work, we have developed a novel strategy to prepare hybrid nanostructures with controlled release properties towards khellin by exploiting the electrostatic interactions between chitosan and halloysite nanotubes (HNT). Firstly, khellin was loaded into the HNT lumen by the vacuum-assisted procedure. The drug confinement within the halloysite cavity has been proved by water contact angle experiments on the HNT/khellin tablets. Therefore, the loaded nanotubes were coated with chitosan as a consequence of the attractions between the cationic biopolymer and the halloysite outer surface, which is negatively charged in a wide pH range. The effect of the ionic strength of the aqueous medium on the coating efficiency of the clay nanotubes was investigated. The surface charge properties of HNT/khellin and chitosan/HNT/khellin nanomaterials were determined by ζ potential experiments, while their morphology was explored through Scanning Electron Microscopy (SEM). Water contact angle experiments were conducted to explore the influence of the chitosan coating on the hydrophilic/hydrophobic character of halloysite external surface. Thermogravimetry (TG) experiments were conducted to study the thermal behavior of the composite nanomaterials. The amounts of loaded khellin and coated chitosan in the hybrid nanostructures were estimated by a quantitative analysis of the TG curves. The release kinetics of khellin were studied in aqueous solvents at different pH conditions (acidic, neutral and basic) and the obtained data were analyzed by the Korsmeyer–Peppas model. The release properties were interpreted on the basis of the TG and ζ potential results. In conclusion, this study demonstrates that halloysite nanotubes wrapped by chitosan layers can be effective as drug delivery systems.

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