Lipid Vesicles for the Skin Delivery of Diclofenac: Cerosomes vs. Other Lipid Suspensions

Azarbayjani, Anahita Fathi; Ng, Kai Xin; Chan, Yew Weng; Chan, Sui Yung

doi:10.5681/apb.2015.004

Cited by 7 publications

(2 citation statements)

References 43 publications

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“…Permeation enhancers can achieve more dramatic shifts in permeability, substances added to the API–lipid bilayer system to modify the permeation rate 9 , 10 by various mechanisms such as the disruption of phospholipid packing in the bilayer, solubilization of the API, 11 , 12 or facilitating transport. 13 Permeation enhancers are mostly studied in the context of skin permeation, where the lipidic membrane is easily accessible. Also, there are studies into permeation enhancers for the oral route of administration, e.g., for improving the oral administration of peptides.…”

Section: Introductionmentioning

confidence: 99%

Computational Prodrug Design Methodology for Liposome Formulability Enhancement of Small-Molecule APIs

et al. 2023

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Encapsulation into liposomes is a formulation strategy that can improve efficacy and reduce side effects of active pharmaceutical ingredients (APIs) that exhibit poor biodistribution or pharmacokinetics when administered alone. However, many APIs are unsuitable for liposomal formulations intended for parenteral administration due to their inherent physicochemical properties�lipid bilayer permeability and water−lipid equilibrium partitioning coefficient. Too high permeability results in premature leakage from liposomes, while too low permeability means the API is not able to pass across biological barriers. There are several options for solving this issue: (i) change of the lipid bilayer composition, (ii) addition of a permeability enhancer, or (iii) modification of the chemical structure of the API to design a prodrug. The latter approach was taken in the present work, and the effect of small changes in the molecular structure of the API on its permeation rate across a lipidic bilayer was systematically explored utilizing computer simulations. An in silico methodology for prodrug design based on the COSMOperm approach has been proposed and applied to four APIs (abiraterone, cytarabine, 5-fluorouracil, and paliperidone). It is shown that the addition of aliphatic hydrocarbon chains via ester or amide bonds can render the molecule more lipophilic and increase its permeability by approximately 1 order of magnitude for each 2 carbon atoms added, while the formation of fructose adducts can provide a more hydrophilic character to the molecule and reduce its lipid partitioning. While partitioning was found to depend only on the size and type of the added group, permeability was found to depend also on the added group location. Overall, it has been shown that both permeability and lipid partitioning coefficient can be systematically shifted into the desired liposome formulability window by appropriate group contributions to the parental drug. This can significantly increase the portfolio of APIs for which liposome or lipid nanoparticle formulations become feasible.

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Section: Introductionmentioning

confidence: 99%

Computational Prodrug Design Methodology for Liposome Formulability Enhancement of Small-Molecule APIs

et al. 2023

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“…When likened to liposomes and niosomes in liquid media, transferosomes have asserted the greatest colloidal stability in the form of zeta potential [ 5 ]. Transferosomes have also displayed excellent colloidal stability (a sign of no aggregation) of up to three months at both 4 and 25 °C, whereas niosomes and liposomes have exhibited worse physical stability with a higher propensity for aggregation [ 6 , 7 ]. This fact explains why, to extend the shelf-life of the product, the majority of marketed liposomal formulations are in freeze-dried powders [ 8 ].…”

Section: Introductionmentioning

confidence: 99%

Box–Behnken Design: Optimization of Proanthocyanidin-Loaded Transferosomes as an Effective Therapeutic Approach for Osteoarthritis

Tamilarasan

Begum

Anitha³

et al. 2022

Nanomaterials

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Transferosomes are one of the vesicular carriers that have received extensive research and attention recently because of their capacity to get beyond the barriers posed by the stratum corneum to penetration. The intent of the current study is to optimize and evaluate proanthocyanidin (PAC) containing transferosomal transdermal gels. PAC-containing transferosomes were prepared using the film hydration method and then loaded into a 4% methylcellulose gel. A 23 Box–Behnken design was used to optimize the PAC-loaded transferosomal gel, where the effects of phospholipid 90 G (X1), Tween 80 (X2), and sonication time (X3) were evaluated. The formulation factors, such as the drug entrapment efficiency percentage (PEE) and in vitro drug release, were characterized. A PEE of 78.29 ± 1.43% and a drug release in vitro at 6 h of 24.2 ± 1.25% were obtained. The optimized transferosomal-loaded proanthocyanidin (OTP) formulation penetrated the porcine skin at an excellent rate (0.123 ± 0.0067 mg/cm2/h). Stability tests were conducted for OTP to predict the effects of various temperature conditions on the physical appearance, drug content, and PEE for periods of 15, 30, and 45 days. Finally, this transferosomal system for transdermal PAC delivery may be a suitable alternative to the conventional treatment for osteoarthritis.

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Therapeutic Implications of Nanopharmaceuticals in Skin Delivery

Mota

Santos-Rebelo

Almeida

et al. 2020

Nanopharmaceuticals: Principles and Applications Vol. 1

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Lipid Vesicles for the Skin Delivery of Diclofenac: Cerosomes vs. Other Lipid Suspensions

Cited by 7 publications

References 43 publications

Computational Prodrug Design Methodology for Liposome Formulability Enhancement of Small-Molecule APIs

Computational Prodrug Design Methodology for Liposome Formulability Enhancement of Small-Molecule APIs

Box–Behnken Design: Optimization of Proanthocyanidin-Loaded Transferosomes as an Effective Therapeutic Approach for Osteoarthritis

Therapeutic Implications of Nanopharmaceuticals in Skin Delivery

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