Ionic co-aggregates (ICAs) based oral drug delivery: Solubilization and permeability improvement

Zheng, Xianzi; Fang, Zhezheng; Huang, Weizi; Qi, Jianping; Dong, Xiaochun; Zhao, Weili; Wu, Wei; Lü, Yi

doi:10.1016/j.apsb.2022.04.011

Cited by 20 publications

(3 citation statements)

References 53 publications

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“…IL-based formulations are also considered potential alternatives for the oral delivery of small molecular hydrophobic drugs. For example, the choline oleate IL-based formulation significantly enhances the absorption of PTX delivered orally compared with the marketed chromophore EL-based formulation [102]. Similarly, the CAGE 1:2-containing formulation has been investigated for the oral delivery of hydrophobic drug sorafenib, resulting in an IL-based formulation with a peak plasma concentration, drug elimination half-life, and mean absorption time 2.2-, 2-, and 1.6-fold higher, respectively, than those of the parent drug suspension (Figure 7A) [97].…”

Section: Bio-ils In Oral Formulation and Deliverymentioning

confidence: 99%

Recent Advances in Biocompatible Ionic Liquids in Drug Formulation and Delivery

et al. 2023

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The development of effective drug formulations and delivery systems for newly developed or marketed drug molecules remains a significant challenge. These drugs can exhibit polymorphic conversion, poor bioavailability, and systemic toxicity, and can be difficult to formulate with traditional organic solvents due to acute toxicity. Ionic liquids (ILs) are recognized as solvents that can improve the pharmacokinetic and pharmacodynamic properties of drugs. ILs can address the operational/functional challenges associated with traditional organic solvents. However, many ILs are non-biodegradable and inherently toxic, which is the most significant challenge in developing IL-based drug formulations and delivery systems. Biocompatible ILs comprising biocompatible cations and anions mainly derived from bio-renewable sources are considered a green alternative to both conventional ILs and organic/inorganic solvents. This review covers the technologies and strategies developed to design biocompatible ILs, focusing on the design of biocompatible IL-based drug formulations and delivery systems, and discusses the advantages of these ILs in pharmaceutical and biomedical applications. Furthermore, this review will provide guidance on transitioning to biocompatible ILs rather than commonly used toxic ILs and organic solvents in fields ranging from chemical synthesis to pharmaceutics.

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Section: Bio-ils In Oral Formulation and Deliverymentioning

confidence: 99%

Recent Advances in Biocompatible Ionic Liquids in Drug Formulation and Delivery

et al. 2023

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“…Our group has successfully developed a novel technique to measure in vivo dissolution by monitoring residual drug particles in the gastrointestinal tract (GIT) of rats through fluorescence-based live imaging . The core of the technique stems from aggregation-caused quenching (ACQ) fluorophores that are physically embedded in crystal lattice to illuminate drug particles. − Once the ACQ fluorophores were released due to particle dissolution and came into contact with water, the dye molecules aggregated via π–π stacking, leading to complete quenching of fluorescence. − This “on-to-off” switching enables the identification of intact drug particles by eliminating the interference from free fluorophores. − The fluorescent intensity was linearly correlated with the concentration of the residual drug particles during dissolution. The residual percentage of fluorescence in rats was recorded with time, which was converted to in vivo dissolution by the difference from 100% (Figure ).…”

Section: Introductionmentioning

confidence: 99%

Establishment of In Vitro Dissolution Based on Similarity with In Vivo Dissolution: A Case Study on Aripiprazole

Man

Yang

et al. 2023

Mol. Pharmaceutics

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In vitro dissolution that predicts the in vivo performance of solid preparations is extremely important in formulation optimization. Fraction absorbed (F a ) has been used to screen in vitro dissolution protocols based on the idea of in vitro−in vivo correlation (IVIVC) but failed to increase the success rate due to the inaccuracy of the F a . The essence of IVIVC is the correlation between in vitro dissolution and in vivo dissolution. We tried to establish in vitro dissolution protocol via similarity with in vivo dissolution using aripiprazole (APZ) as a model drug. Hybrid APZ crystals (APZ-HCs) were prepared by physically embedding aggregation-caused quenching (ACQ) fluorophores inside the lattice to measure the in vivo dissolution. The process did not change the physicochemical properties and crystallinity of APZ. The fluorophore illuminated APZ crystals but was quenched upon dissolution of APZ-HCs in aqueous media, enabling monitoring intact APZ-HCs in real-time. The good correlation between fluorescent quenching and dissolution of APZ-HCs justified reliable quantification of intact APZ crystals. The residual percentage of fluorescence intensity in rats treated by APZ-HCs was recorded with time, which was converted to in vivo dissolution by the difference from 100%. The in vivo dissolution was validated with the F a . The in vitro dissolution profile of APZ was set up via a similarity factor larger than 50 in comparison with the in vivo dissolution. The study provides a novel idea and method to establish in vitro dissolution protocol.

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“…Lipid-based formulations have been a traditional solution to the oral delivery of BC IV drugs [ 14 , 15 , 16 ]. The underlying mechanism is related to intestinal lipolysis, which converts lipids into colloidal structures, including multilamellar and unilamellar vesicles, mixed micelles, and micelles, together with bile salts, phospholipids, and cholesterol [ 17 , 18 ].…”

Section: Introductionmentioning

confidence: 99%

Pickering Emulsions Enhance Oral Bioavailability of Curcumin Nanocrystals: The Effect of Oil Types

et al. 2023

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Nanocrystals (NCs) have the potential to enhance the oral bioavailability of Class IV drugs in the Biopharmaceutical Classification System (BCS) due to the absorption of the intact crystals. The performance is compromised by the dissolution of NCs. Drug NCs have recently been adopted as solid emulsifiers to prepare nanocrystal self-stabilized Pickering emulsions (NCSSPEs). They are advantageous in high drug loading and low side effects due to the specific drug loading mode and the absence of chemical surfactants. More importantly, NCSSPEs may further enhance the oral bioavailability of drug NCs by impeding their dissolution. This is especially true for BCS IV drugs. In this study, curcumin (CUR), a typical BCS IV drug, was adopted to prepare CUR-NCs stabilized Pickering emulsions using either indigestible (isopropyl palmitate, IPP) or digestible (soybean oil, SO) oils, i.e., IPP-PEs and SO-PEs. The optimized formulations were spheric with CUR-NCs adsorbed on the water/oil interface. The CUR concentration in the formulation reached 20 mg/mL, which was far beyond the solubility of CUR in IPP (158.06 ± 3.44 μg/g) or SO (124.19 ± 2.40 μg/g). Moreover, the Pickering emulsions enhanced the oral bioavailability of CUR-NCs, being 172.85% for IPP-PEs and 152.07% for SO-PEs. The digestibility of the oil phase affected the amounts of CUR-NCs that remained intact in lipolysis and, thus, the oral bioavailability. In conclusion, converting NCs into Pickering emulsions provides a novel strategy to enhance the oral bioavailability of CUR and BCS IV drugs.

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Ionic co-aggregates (ICAs) based oral drug delivery: Solubilization and permeability improvement

Cited by 20 publications

References 53 publications

Recent Advances in Biocompatible Ionic Liquids in Drug Formulation and Delivery

Recent Advances in Biocompatible Ionic Liquids in Drug Formulation and Delivery

Establishment of In Vitro Dissolution Based on Similarity with In Vivo Dissolution: A Case Study on Aripiprazole

Pickering Emulsions Enhance Oral Bioavailability of Curcumin Nanocrystals: The Effect of Oil Types

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