Development and evaluation of long-circulating nanoparticles loaded with betulinic acid for improved anti-tumor efficacy

Saneja, Ankit; Kumar, Robin; Singh, Amarinder; Dubey, Rajesh Kumar; Mintoo, Mubashir J.; Singh, Gurdarshan; Mondhe, Dilip M.; Panda, Amulya K.; Gupta, Prem N.

doi:10.1016/j.ijpharm.2017.08.076

Cited by 58 publications

(36 citation statements)

References 46 publications

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“…34,35 The PEGylated nanoparticles are able to protect the carried drug from biological and chemical degradation, increasing the systemic retention periods of the drug in vivo. 36 In this study, we generated DBZ-NLC and DBZ-PEG-NLC and found that both DBZ-NLC and DBZ-PEG-NLC had similar PIs and good drug entrapment efficiency and LC. In addition, both DBZ-PEG-NLC and DBZ-NLC displayed a biphasic pattern of DBZ release in vitro.…”

Section: Discussionmentioning

confidence: 89%

Tanshinol borneol ester on nanostructured lipid carriers has longer brain and systemic effector retention and better antioxidant activity in vivo

Yuan¹,

Fei²,

Sun³

et al. 2018

IJN

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BackgroundTanshinol borneol ester (DBZ) is a hybrid of danshensu (DSS) and borneol and has anti-ischemic activity in animals. However, its low water solubility and short half-life limit its clinical application.MethodsWe prepared polyethylene glycol (PEG)-modified and DBZ-loaded nanostructured lipid carriers (DBZ-PEG-NLC) and DBZ-NLC, and examined their physical characteristics, such as particle size, zeta potential, entrapment efficiency and drug loading. The in vitro stability and pharmacokinetics in rats as well as antioxidant activity of DBZ-PEG-NLC and DBZ-NLC in a C57BL/6 mouse model of ischemia/reperfusion-related brain injury were investigated. The levels of DBZ and its hydrolyzed DSS in rat plasma and brain microdialysates were determined by liquid chromatography–mass spectroscopy/mass spectroscopy analysis.ResultsWe found that the mean particle size and entrapment efficacy of DBZ-PEG-NLC were similar to that of DBZ-NLC. The DBZ-PEG-NLC, like DBZ-NLC, released DBZ in a biphasic manner with initially burst release and then prolonged slow release in vitro. Intravenous injection of DBZ-PEG-NLC resulted in significantly higher levels and longer retention periods of DBZ and DSS in plasma and the brains than DBZ-NLC and DBZ in rats. Finally, treatment with DBZ-PEG-NLC achieved a better antioxidant activity than DBZ or DBZ-NLC in mouse model of ischemia/reperfusion by reducing the levels of brain malondialdehyde, but increasing the levels of brain superoxide dismutase and glutathione.ConclusionDBZ-PEG-NLC is a preferable option to deliver DBZ for sustainable release of DSS and borneol in vivo, and may serve as a promising drug for effective therapy of ischemic cardiovascular and cerebrovascular diseases.

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Section: Discussionmentioning

confidence: 89%

Tanshinol borneol ester on nanostructured lipid carriers has longer brain and systemic effector retention and better antioxidant activity in vivo

Yuan¹,

Fei²,

Sun³

et al. 2018

IJN

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“…Current therapies used for leishmaniasis encountered some difficulties due to their high toxicity and low water solubility (8,10,(20)(21)(22)(23). Nowadays nanocarriers were successful in solving these problems (5).…”

Section: Discussionmentioning

confidence: 99%

In Vivo Therapeutic Effects of Four Synthesized Antileishmanial Nanodrugs in the Treatment of Leishmaniasis

Mehrizi

Mosaffa

Hoseini

et al. 2018

Arch Clin Infect Dis

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Background: Nowadays, nanocarriers are used for leishmaniasis treatment due to development of drug resistance and several side effects with conventional therapeutics. Objectives: In this study we aimed to evaluate in vivo effects of four synthesized nanodrugs including amphotericin B-nanochitosan (AK), betulinic acid-nanochitosan (BK), amphotericin B-dendrimer (AD), and betulinic acid-dendrimer (BD) in the treatment of Leishmania major infection (L. major) in mice model by using pathological analyses to choose the most effective nanodrug in leishmaniasis. Methods: The four nanodrugs efficacy in the improvement of L. major lesion in a mice model was evaluated by using pathological analyses including measurement of organs size and parasite number. Additionally, the nanodrugs toxicity was evaluated by measurement of various blood factors. Results: The histopathological results of the present study showed that BK, at the dose of 20 mg/kg, and AK, at the dose of 10 mg/kg, were more effective in decreasing the parasite number in the kidney, liver, and spleen. Moreover, BK20 mg/kg and AK10 mg/kg decreased the organs size significantly while AD50 mg/kg and BD40 mg/kg were less effective. However, none of the four nanodrugs had increased the blood factors and they were not toxic. Conclusions: Overall, the pathologic findings of various mice organs treated with different formulations showed that AK10 mg/kg and BK20 mg/kg were more effective in recovery of L. major's pathological effects in comparison to AD50 mg/kg and BD40 mg/kg. Therefore, it seems that AK and BK, in this mentioned dosage, could be considered as a proper candidate for treatment of leishmaniasis.

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“…Moreover, modifying the surface of PLGA nanocarriers with stealth polymers, such as polyethylene glycol (PEG) or CS, could prolong the systemic circulation time owing to the reduction of protein opsonization, which leads to a decrease in nonspecific uptake toward normal tissues . Considering these facts, in a recent study, we developed BA encapsulated in monomethoxy polyethylene glycol–modified poly( d,l ‐lactide‐coglycolide) (mPEG–PLGA) NPs for improving its in vivo half‐life and anticancer efficacy . Our findings indicated that the developed mPEG–PLGA NPs are suitable to be used for the delivery of BA.…”

Section: Nanoformulations For Betulinic Acid Deliverymentioning

confidence: 97%

Therapeutic applications of betulinic acid nanoformulations

Saneja

Arora

Kumar

et al. 2018

Annals of the New York Academy of Sciences

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Betulinic acid (BA), a naturally occurring plant-derived pentacyclic triterpenoid, has gained attention in recent years owing to its broad-spectrum biological and medicinal properties. Despite the pharmacological activity of BA, it has been associated with some drawbacks, such as poor aqueous solubility and short half-life in vivo, which limit therapeutic application. To solve these problems, much work in recent years has focused on enhancing BA's aqueous solubility, half-life, and efficacy by using nanoscale drug delivery systems. Several different kinds of nanoscale delivery systems-including polymeric nanoparticles, magnetic nanoparticles, liposomes, polymeric conjugates, nanoemulsions, cyclodextrin complexes, and carbon nanotubes-have been developed for the delivery of BA. Here, we focus on the recent developments of novel nanoformulations used to deliver BA in order to improve its efficacy.

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Development and evaluation of long-circulating nanoparticles loaded with betulinic acid for improved anti-tumor efficacy

Cited by 58 publications

References 46 publications

Tanshinol borneol ester on nanostructured lipid carriers has longer brain and systemic effector retention and better antioxidant activity in vivo

Tanshinol borneol ester on nanostructured lipid carriers has longer brain and systemic effector retention and better antioxidant activity in vivo

In Vivo Therapeutic Effects of Four Synthesized Antileishmanial Nanodrugs in the Treatment of Leishmaniasis

Therapeutic applications of betulinic acid nanoformulations

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