Formulation of dried lignans nanosuspension with high redispersibility to enhance stability, dissolution, and oral bioavailability

Shen, Gang; Cheng, Lan; Wang, Liqiang; Zhang, Lihong; Shen, Biao; Liao, Wei-Bo; Li, Juanjuan; Zheng, Juan; Xu, Rong; Yuan, Hailong

doi:10.1016/s1875-5364(16)30090-5

Cited by 8 publications

(2 citation statements)

References 36 publications

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“…High supersaturation was needed in order to produce small and uniform particles to accelerate a nucleation rate greater than the rate of crystal growth. However, when the drug concentration was excessive, a large number of nuclei quickly formed on the interface of solid phase and liquid phase and slowed the diffusion from solvent to antisolvent, leading to particle adhesion and larger particle production [40]. Furthermore, the increasing drug concentration may cause the increasing of the viscosity of the solutions and avoiding particle diffusion [41].…”

Section: Resultsmentioning

confidence: 99%

Enhanced Intradermal Delivery of Nanosuspensions of Antifilariasis Drugs Using Dissolving Microneedles: A Proof of Concept Study

2019

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Conventional oral administration of antifilariasis drugs results in nonspecific targeting of the drugs and the intradermal delivery of nanoparticles with sizes of <100 nm could be used to improve lymphatic uptake. This study investigated the combination of nanosuspension and dissolving microneedles (MN-NS) as an alternative intradermal delivery approach for the delivery of antifilariasis drugs, namely doxycycline, albendazole, and ivermectin. NS were fabricated and optimized using a bottom-up technique. The NS were then incorporated into the MN arrays. The optimized NS were <100 nm in diameter. Furthermore, MN-NS had suitable mechanical strength and insertion capabilities. The dermatokinetic study revealed that the delivery of drugs into the dermis of excised neonatal porcine skin by MNs was significantly higher than that from a needle-free patch, with 29.29 ± 4.65%, 31.54 ± 5.35%, and 34.54 ± 4.98% of doxycycline, albendazole sulfoxide, and ivermectin retained in the dermis after 24 h. The results presented here serve as proof of concept for the significant enhancement of drug retention times in the dermis, following their formulation into NS and delivery via MN. Leading on from these studies, future work must investigate in vivo lymphatic pharmacokinetic profiling of drugs formulated into NS, in a suitable animal model.

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Section: Resultsmentioning

confidence: 99%

Enhanced Intradermal Delivery of Nanosuspensions of Antifilariasis Drugs Using Dissolving Microneedles: A Proof of Concept Study

2019

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“…Previous studies have reported that HPS and its major lignan components have hepatoprotective effects ( Shen et al, 2015 ; Shen et al, 2016 ; Feng et al, 2018 ). However, the hepatoprotective effects of HPP have been seldomly investigated.…”

Section: Discussionmentioning

confidence: 99%

Total cucurbitacins from Herpetospermum pedunculosum pericarp do better than Hu-lu-su-pian (HLSP) in its safety and hepatoprotective efficacy

Liu,

Xu,

et al. 2024

Front. Pharmacol.

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The pericarp of Herpetospermum pedunculosum (HPP) has traditionally been used for treating jaundice and hepatitis. However, the specific hepatoprotective components and their safety/efficacy profiles remain unclear. This study aimed to characterize the total cucurbitacins (TCs) extracted from HPP and evaluate their hepatoprotective potential. As a reference, Hu-lu-su-pian (HLSP), a known hepatoprotective drug containing cucurbitacins, was used for comparison of chemical composition, effects, and safety. Molecular networking based on UHPLC-MS/MS identified cucurbitacin B, isocucurbitacin B, and cucurbitacin E as the major components in TCs, comprising 70.3%, 26.1%, and 3.6% as determined by RP-HPLC, respectively. TCs treatment significantly reversed CCl4-induced metabolic changes associated with liver damage in a dose-dependent manner, impacting pathways including energy metabolism, oxidative stress and phenylalanine metabolism, and showed superior efficacy to HLSP. Safety evaluation also showed that TCs were safe, with higher LD50 and no observable adverse effect level (NOAEL) values than HLSP. The median lethal dose (LD50) and NOAEL values of TCs were 36.21 and 15 mg/kg body weight (BW), respectively, while the LD50 of HLSP was 14 mg/kg BW. In summary, TCs extracted from HPP demonstrated promising potential as a natural hepatoprotective agent, warranting further investigation into synergistic effects of individual cucurbitacin components.

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Solubility Enhancement Techniques for Natural Product Delivery

Jain

Chella

2020

Sustainable Agriculture Reviews

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Formulation of dried lignans nanosuspension with high redispersibility to enhance stability, dissolution, and oral bioavailability

Cited by 8 publications

References 36 publications

Enhanced Intradermal Delivery of Nanosuspensions of Antifilariasis Drugs Using Dissolving Microneedles: A Proof of Concept Study

Enhanced Intradermal Delivery of Nanosuspensions of Antifilariasis Drugs Using Dissolving Microneedles: A Proof of Concept Study

Total cucurbitacins from Herpetospermum pedunculosum pericarp do better than Hu-lu-su-pian (HLSP) in its safety and hepatoprotective efficacy

Solubility Enhancement Techniques for Natural Product Delivery

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