Eudragit S-100 Surface Engineered Nanostructured Lipid Carriers for Colon Targeting of 5-Fluorouracil: Optimization and In Vitro and In Vivo Characterization

Borderwala, Kruti; Rathod, Sachin; Yadav, Sarita; Vyas, Bhavin; Shah, Pranav

doi:10.1208/s12249-021-02099-3

Cited by 18 publications

(6 citation statements)

References 47 publications

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“…In the case of the 5-FU-compritol ® physical mixture, characteristic peaks of the drug at 3136 cm −1 , 1640 cm −1 and 1273 cm −1 were also present, compritol ® peaks at 2922 cm −1 , 1707 cm −1 , and 1592 cm −1 were present as shown in fig. 11(b) and table 6 [57].…”

Section: Pre-formulation Studies With Excipientsmentioning

confidence: 96%

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 Excipientsmentioning

confidence: 96%

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

et al. 2022

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“…The latter, an oligosaccharide that resists degradation in the stomach and small intestine, can be broken down by enzymes produced by resident colonic bacteria, thus allowing drug release. Eudragit was also used to engineered NLCs for the colon targeting of 5-Fluorouracil; its effectiveness in terms of higher bioavailability and longer release was confirmed in both in vitro and in vivo (in rats) tests [ 128 ]. Although less exploited, other molecules exist which can intrinsically enable pH sensitivity in a formulation.…”

Section: Resultsmentioning

confidence: 99%

Targeting the Gut: A Systematic Review of Specific Drug Nanocarriers

Garbati,

Picco,

Magrassi

et al. 2024

Pharmaceutics

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The intestine is essential for the modulation of nutrient absorption and the removal of waste. Gut pathologies, such as cancer, inflammatory bowel diseases (IBD), irritable bowel syndrome (IBS), and celiac disease, which extensively impact gut functions, are thus critical for human health. Targeted drug delivery is essential to tackle these diseases, improve therapy efficacy, and minimize side effects. Recent strategies have taken advantage of both active and passive nanocarriers, which are designed to protect the drug until it reaches the correct delivery site and to modulate drug release via the use of different physical–chemical strategies. In this systematic review, we present a literature overview of the different nanocarriers used for drug delivery in a set of chronic intestinal pathologies, highlighting the rationale behind the controlled release of intestinal therapies. The overall aim is to provide the reader with useful information on the current approaches for gut targeting in novel therapeutic strategies.

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Section: Application Of Nasal Delivery Of Nucleic Acid Based Therapeu...mentioning

confidence: 99%

“…5-Fluorouracil, a nucleoside analog has been employed either alone or in synergism with other anticancer drugs to treat various types of malignancies (Miura et al, 2010;Borderwala et al, 2021). Sakane et al (1999) studied the brain uptake of 5-FU in Wistar rats following intravenous and nasal application.…”

Section: Nucleoside Analoguesmentioning

confidence: 99%

Intranasal delivery: An attractive route for the administration of nucleic acid based therapeutics for CNS disorders

Shah

Lalan²,

Barve

2022

Front. Pharmacol.

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The etiologies of several cardiovascular, inflammatory, neurological, hereditary disorders, cancer, and infectious diseases have implicated changes in the genetic set up or genetic mutations as the root cause. Nucleic acid based therapeutics (NBTs) is a new class of biologics that are known to regulate gene expression at the transcriptional and post-transcriptional level. The NBTs include oligonucleotides, nucleosides, antisense RNA, small interfering RNAs, micro RNA etc. In recent times, this new category of biologics has found enormous potential in the management of cardiovascular, inflammatory, neurological disorders, cancer, infectious diseases and organ transplantation. However, the delivery of NBTs is highly challenging in terms of target specificity (intracellular delivery), mononuclear phagocyte system uptake, stability and biodistribution. Additionally, management of the above mentioned disorders require regular and intrusive therapy making non-invasive routes preferable in comparison to invasive routes like parenteral. The nasal route is garnering focus in delivery of NBTs to the brain in the management of several CNS disorders due to the associated merits such as non-invasiveness, possibility of chronic delivery, improved patient compliance, avoidance of hepatic and gastrointestinal metabolism as well as ability to bypass the BBB. Hence in recent times, this route has been sought by the reserachers as an alternative to parenteral therapy for the delivery of several NBTs. This review shall focus on an array of NBTs delivered through nasal route, their challenges, applications and opportunities. The novel delivery systems for incorporating NBTs; their targeting strategies shall be critically reviewed. The challenges towards regulatory approvals and commercialization shall also be discussed at large. Comparison of learnings derived from the success and barriers in nasal delivery of NBTs will help in identification of futuristic opportunities for their translation from bench to bedside.

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Eudragit S-100 Surface Engineered Nanostructured Lipid Carriers for Colon Targeting of 5-Fluorouracil: Optimization and In Vitro and In Vivo Characterization

Cited by 18 publications

References 47 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

Targeting the Gut: A Systematic Review of Specific Drug Nanocarriers

Intranasal delivery: An attractive route for the administration of nucleic acid based therapeutics for CNS disorders

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