Preparation and Characterization of Ivabradine HCl Transfersomes for Enhanced Transdermal Delivery

Balata, Gehan F.; Faisal, Mennatullah M.; Elghamry, Hanaa A.; Sabry, Shereen A.

doi:10.1016/j.jddst.2020.101921

Cited by 50 publications

(42 citation statements)

References 39 publications

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“…This occurred because the unentrapped BBR in the vesicle surface passed through the skin earlier, while the entrapped BBR diffused slowly from the vesicle and penetrated through the skin. This result was in line with the study by Balata et al (2020), which stated that the initial rapid release phase was observed from 0 to 4 hours after transfersomes were applied.…”

Section: In Vitro Penetration Study Of Bbr Transfersomal Emulgelsupporting

confidence: 92%

Development of transfersomal emulgel to enhance the permeation of berberine chloride for transdermal delivery

Fitria¹,

Surini²,

Iswandana³

2022

J App Pharm Sci

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The low penetration of berberine chloride (BBR) through the skin is due to its hydrophilic characteristic. Therefore, this study aims to enhance the penetration of BBR using transfersomal emulgel for transdermal delivery. Four formulations used were prepared by varying the ratio of the main ingredient concentrations and the transfersomes were also prepared by a solvent evaporation method. Subsequently, the BBR transfersomes were formulated into emulgel and in vitro penetration was carriexd out using Franz diffusion cells for 12 hours. The results showed that the best transfersome formula was F2 transfersomes, which had a deformable spherical shape, particle size (Z Average ) of 153.9 ± 2.07 nm, polydispersity index of 0.103 ± 0.033, zeta potential of −32.47 ± 0.551 mV, and entrapment efficiency of 93.97 ± 0.31%. Furthermore, the BBR transfersomal emulgel showed yellow, good homogeneity, and range from pH 7.2 to 7.4. All the formulae had drug content that ranged from 98.34% to 105.87% and the BBR penetration was much enhanced by transfersomal emulgel F2 compared to the nontransfersomal emulgel by 3.8-fold. This study showed that the transfersomal emulgel formulation provides higher levels of BBR permeation through the skin.

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Section: In Vitro Penetration Study Of Bbr Transfersomal Emulgelsupporting

confidence: 92%

Development of transfersomal emulgel to enhance the permeation of berberine chloride for transdermal delivery

Fitria¹,

Surini²,

Iswandana³

2022

J App Pharm Sci

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“…The easiest way to change the transfersome properties is to vary the ratio of components and type of surfactant [153]. For example, 12 systems with different surfactants, drug: phosphatidylcholine and surfactant:phosphatidylcholine ratios were studied in [180]. Adding sodium lauryl sulphate to the system led to an increase of EE% of the hydrophilic drug ivabradine hydrochloride compared to cases with Tween 80 and cetrimide.…”

Section: Transfersomes and Transethosomesmentioning

confidence: 99%

“…It is possible to achieve the necessary size, charge and EE% by varying the ratio of components. In [181], three phospholipid:surfactant ratios were varied (90:10, 85:15, and 75:25) and, according to the results, a components ratio of 85:15 proved to be optimal in all parameters, while in [180] the system with ratio of 75:25 had the best size and charge as well as high EE% values and prolonged substrate release.…”

Section: Transfersomes and Transethosomesmentioning

confidence: 99%

Self-Assembling Drug Formulations with Tunable Permeability and Biodegradability

et al. 2021

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This review focuses on key topics in the field of drug delivery related to the design of nanocarriers answering the biomedicine criteria, including biocompatibility, biodegradability, low toxicity, and the ability to overcome biological barriers. For these reasons, much attention is paid to the amphiphile-based carriers composed of natural building blocks, lipids, and their structural analogues and synthetic surfactants that are capable of self-assembly with the formation of a variety of supramolecular aggregates. The latter are dynamic structures that can be used as nanocontainers for hydrophobic drugs to increase their solubility and bioavailability. In this section, biodegradable cationic surfactants bearing cleavable fragments are discussed, with ester- and carbamate-containing analogs, as well as amino acid derivatives received special attention. Drug delivery through the biological barriers is a challenging task, which is highlighted by the example of transdermal method of drug administration. In this paper, nonionic surfactants are primarily discussed, including their application for the fabrication of nanocarriers, their surfactant-skin interactions, the mechanisms of modulating their permeability, and the factors controlling drug encapsulation, release, and targeted delivery. Different types of nanocarriers are covered, including niosomes, transfersomes, invasomes and chitosomes, with their morphological specificity, beneficial characteristics and limitations discussed.

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“… 5 The drug has excellent physicochemical characteristics including its high solubility (50 mg/mL), suitable partition coefficient (3.17) and small molecular weight (468.6 g/mol). 6 , 7 Unfortunately, ivabradine has significantly low oral bioavailability (≈ 40%) due to its extensive first-pass metabolism that yields inactive metabolites. 8 Ivabradine is a substrate for the CYP3A4 enzyme system which is mainly present in the gut and the liver.…”

Section: Introductionmentioning

confidence: 99%

“…13 Recently, Balata et al developed transfersomes loaded with ivabradine utilizing either tween 80, sodium lauryl sulfate or cetrimide as stabilizers and permeation enhancers mixed in different ratios with the drug and phospholipid. 6 The optimized transfersomal formula was incorporated into a film composed of hydroxypropyl methylcellulose and starch in ratio 1:1 w/w. The developed nanostructured transdermal film showed improved permeability and retention compared to the unformulated ivabradine.…”

Section: Introductionmentioning

confidence: 99%

Simultaneous Optimization of Oral and Transdermal Nanovesicles for Bioavailability Enhancement of Ivabradine Hydrochloride

Naguib¹,

Elsayed²,

Teaima³

2021

IJN

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Purpose Ivabradine hydrochloride is selective pacemaker current (I f ) ion channel inhibitor used in case of chronic heart failure (CHF) with superior efficacy and lower side effects than most β-blockers. However, the drug suffers from low bioavailability (≈40%) due to extensive first-pass metabolism. Hence, this work aims to formulate nanovesicular platforms to enhance their bioavailability both orally and transdermally. Materials and Methods A central composite face-centered design was employed to formulate the nanovesicles, both phosphatidylcholine: drug ratio and percentage of pluronic F68 were used as independent variables. The nine developed formulae were characterized in terms of vesicle size (nm), polydispersity index, zeta potential (mV), entrapment efficiency (%). Decreasing vesicle size, increasing negative value of the zeta potential, and increasing entrapment efficiency were the chosen constraints to optimize the engineered nanovesicles. The candidate formula was subjected to further investigation including lyophilization, loading into carbopol gel, in vitro release, imaging with a transmission electron microscope, histopathological examination, in vitro cytotoxicity study and in vivo pharmacokinetics. Results The optimized nanovesicular formula was composed of lipid: drug ratio of 3.91:1 and 100% pluronic as a stabilizer. It has particle size, zeta potential and entrapment efficiency of 337.6 nm, −40.5 mV and 30.5, respectively. It was then lyophilized in the presence of 5% trehalose as a cryoprotectant, dispersed in 0.5% carbopol to develop the transdermal gel. The two different forms of the candidate formula (lyophilized and gel form) displayed sustained drug release in comparison to drug solution. The histopathological and cytotoxicity studies showed that the optimized formula was safe and highly biocompatible. The pharmacokinetics parameters measured declared a higher C max and half-life of both formulae in comparison to market product (Procoralan ® ) with a 2.54- and 1.85-folds increase in bioavailability, respectively. Conclusion Hence, the developed nanovesicles can be reported as the first nanoplatforms to be used for simultaneous ivabradine delivery by both oral and topical routes with enhanced oral and transdermal drug delivery. The developed nanoplatforms hence can be further used to formulate other drugs that suffer from low bioavailability due to extensive first-pass metabolism.

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Preparation and Characterization of Ivabradine HCl Transfersomes for Enhanced Transdermal Delivery

Cited by 50 publications

References 39 publications

Development of transfersomal emulgel to enhance the permeation of berberine chloride for transdermal delivery

Development of transfersomal emulgel to enhance the permeation of berberine chloride for transdermal delivery

Self-Assembling Drug Formulations with Tunable Permeability and Biodegradability

Simultaneous Optimization of Oral and Transdermal Nanovesicles for Bioavailability Enhancement of Ivabradine Hydrochloride

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