Development, evaluation and biodistribution of stealth liposomes of 5-fluorouracil for effective treatment of breast cancer

Katharotiya, Khushboo; Shinde, Gajanan; Katharotiya, Dhaval; Shelke, Santosh; Patel, Rakesh; Kulkarni, Deepak; Panzade, Prabhakar

doi:10.1080/08982104.2021.1905661

Cited by 18 publications

(4 citation statements)

References 36 publications

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“…11(a) and table 6, there was a minor shift in the drug principal peaks at 3101 cm −1 ,1658 cm −1 ,1465 cm −1 ,1442 cm −1 ,1257 cm −1 and 1338 cm −1 for N-H stretching, C=O bending, C=C stretching, C-F stretching, C-N stretching and pyrimidine bending, respectively. A similar finding was confirmed by Katharotiya et al [56].…”

Section: Pre-formulation Studies With Excipientssupporting

confidence: 86%

Pre-Formulation Study on 5-Fluorouracil and Certain Lipids for Solid Lipid Nanoparticles Preparation

et al. 2022

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Objective: The study's objective involved compatibility studies to investigate the possible interactions between 5-fluorouracil (5-FU) and four different lipids, and the most appropriate lipid was chosen. Differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier Transform Infrared spectroscopy (FT-IR) are used for the compatibility study between 5-FU and several excipients as cholesterol, compritol®, stearic acid, and glycerol monostearate (GMS). Methods: The physical mixture between 5-FU and each lipid was made by mixing of a certain amount of drug with the same amount of lipid. Drug lipid blended mixtures were made by solvent evaporation casting method. 5-FU alone, physical mixture and blended mixture were measured using Differential scanning calorimetry (DSC) to investigate melting peak of drug and effect of each lipid on this melting point, X-ray diffraction (XRD) to observe the crystalline or amorphous state of drug and Fourier Transform Infrared (FT-IR) to determine any chemical interaction between drug and these lipids by observing any shift happened to characteristic peaks related to the drug. Results: 5-FU Tm (280.04 °C) peak appeared in drug-lipid physical mixtures with minor changes in position while this peak disappeared in 5-FU-compritol® and 5-FU-cholesterol blended mixture, indicating that the drug is molecular dispersed. XRD result showed that the crystalline structure of 5-FU was present in physical mixtures with four lipids, while in the 5-FU-compritol® blended mixture, the crystalline state of the drug was disappeared, confirming the DSC result. The FT-IR spectrum of the 5-FU-physical mixtures with four lipids showed that all characteristic peaks of the drug appeared with minor changes. In the case of 5-FU-blended mixtures with mentioned lipids, no chemical interaction occurred between the drug and mentioned lipids except in the drug-stearic acid blended mixture, the N-H peak at 3136.25 cm-1 was disappeared due to amide ester formation. Conclusion: The most appropriate lipids suitable for the preparation of 5-FU solid lipid nanoparticles were GMS and cholesterol.

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Section: Pre-formulation Studies With Excipientssupporting

confidence: 86%

Pre-Formulation Study on 5-Fluorouracil and Certain Lipids for Solid Lipid Nanoparticles Preparation

et al. 2022

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“…The SEM studies revealed that the shape and size of the liposomes were smooth and spherical ( Figure 6 ). These results proved that the spherical shape of vesicles was unaggregated and unilamellar with a smaller size so that there would be uniformity in the release of drug [ 41 ].…”

Section: Resultsmentioning

confidence: 94%

Permeability-Enhanced Liposomal Emulgel Formulation of 5-Fluorouracil for the Treatment of Skin Cancer

Pachauri

Chitme

Visht

et al. 2023

Gels

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The plain 5-fluorouracil (5FU) formulations available in the market are associated with adverse effects such as skin irritation, pruritus, redness, blisters, allergy, and dryness on the site of application. The objective of the present study was to develop a liposomal emulgel of 5FU with increased skin permeability and efficacy using clove oil and eucalyptus oil along with pharmaceutically acceptable carriers, excipients, stabilizers, binders, and additives. A series of seven formulations were developed and evaluated for their entrapment efficiency, in vitro release profile, and cumulative drug release profile. The compatibility of drugs and excipients, as confirmed by FTIR (fourier-transform infrared spectroscopy) and DSC (differential scanning calorimetry) as well as SEM (scanning electron microscopy) and TEM (transmission electron microscopy) studies, revealed that the size and shape of liposomes are smooth and spherical, and the liposomes are non-aggregated. To understand their efficacy, the optimized formulations were evaluated for cytotoxicity using B16-F10 mouse skin melanoma cells. The eucalyptus oil and clove oil-containing preparation significantly produced a cytotoxic effect against a melanoma cell line. The addition of clove oil and eucalyptus oil increased the efficacy of the formulation by improving skin permeability and reducing the dose required for the anti-skin cancer activity.

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“…The polydispersity index (PDI) of all formulations was more than 0.3 and did not correspond to a homogeneous population of colloidal systems [23]. All niosome formulation was characterized by a polydispersed population of particles, with the lowest value of PDI shown by F6 at 0.533, while F3, F4, and F5 have the highest PDI value, between 0.9-1.0, which is considered highly polydisperse with multiple particle size populations [26][27][28].…”

Section: Niosome Size Zeta Potential and Polydispersity Index (Pdi)mentioning

confidence: 95%

Formulation and In Vivo Pain Assessment of a Novel Niosomal Lidocaine and Prilocaine in an Emulsion Gel (Emulgel) of Semisolid Palm Oil Base for Topical Drug Delivery

Shabery

Widodo

Chik

2023

Gels

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This study aimed to formulate semisolid niosomal encapsulated lidocaine and prilocaine using the patented palm oil base Hamin-C® for further characterization and in vivo pain assessment. Seven formulations were initially studied with various chemical compositions. A thin-layer film hydration method was used to produce niosome using a mixture of surfactant (Span® 40 or Span® 60) and cholesterol (CHOL) at a 1:1 ratio, with/without a charge-inducing agent (diacetyl phosphate) (DCP) and with/without labrasol®. Niosome F1 formulation had been identified as the highest %EE achieved, at 53.74 and 55.63% for prilocaine and lidocaine, respectively. Furthermore, NIO-HAMIN F1 emulgel indicated the best formulation with higher permeability of prilocaine and lidocaine compared to the rest of the formulations. The reformulation of optimization of NIO-HAMIN F1 emulgel using a cold process to NIO-HAMIN F1-C emulgel to improve the viscosity resulted in higher diffusion of prilocaine and lidocaine by 5.71 and 33.38%, respectively. In vivo pain perception studies by verbal rating score (VRS) and visual analogue score (VAS) on healthy subjects show a comparable local anesthetic effect between NIO-HAMIN F1-C emulgel and EMLA® cream.

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Development, evaluation and biodistribution of stealth liposomes of 5-fluorouracil for effective treatment of breast cancer

Cited by 18 publications

References 36 publications

Pre-Formulation Study on 5-Fluorouracil and Certain Lipids for Solid Lipid Nanoparticles Preparation

Pre-Formulation Study on 5-Fluorouracil and Certain Lipids for Solid Lipid Nanoparticles Preparation

Permeability-Enhanced Liposomal Emulgel Formulation of 5-Fluorouracil for the Treatment of Skin Cancer

Formulation and In Vivo Pain Assessment of a Novel Niosomal Lidocaine and Prilocaine in an Emulsion Gel (Emulgel) of Semisolid Palm Oil Base for Topical Drug Delivery

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