Lecithin-Based Novel Cationic Nanocarriers (Leciplex) II: Improving Therapeutic Efficacy of Quercetin on Oral Administration

Date, Abhijit A.; Nagarsenker, Mangal S.; Patere, Shilpa; Dhawan, Vivek; Gude, Rajiv P.; Hassan, P. A.; Aswal, Vinod K.; Steiniger, Frank; Thamm, Jana; Fahr, Alfred

doi:10.1021/mp100305h

Cited by 98 publications

(41 citation statements)

References 50 publications

(118 reference statements)

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“…In this situation, external supply of antioxidants is essential to counter balance the dangerous effects of oxidative stress. It is evident that flavanoid antioxidants like quercetin have potential role in ROS scavenging in the pathogenesis of diabetes, which can also delay the oxidative injury and cell death [1][2][3].…”

Section: Introductionmentioning

confidence: 99%

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Development of quercetin nanoformulation and in vivo evaluation using streptozotocin induced diabetic rat model

Chitkara

Nikalaje

Mittal

et al. 2012

Drug Deliv. and Transl. Res.

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Quercetin-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (Qu-NP) were prepared by emulsion-diffusion-evaporation method and characterized as 179.9 ± 11.2 nm in size with 0.128 as polydispersity index, more than 86% drug entrapment efficiency, and zeta potential was -6.06 ± 1.51 mV. D-Trehalose (5% w/v) was found to be a suitable cryoprotectant for lyophilization of Qu-NP, and antioxidant assays indicated that Qu-NP were able to retain the antioxidant property similar to that of free drug at equivalent concentration after formulation development. In vitro release study of Qu-NP showed a controlled release pattern of quercetin. An enhanced oral bioavailability (523% relative increase) was observed in pharmacokinetic study with a 6-day sustained release from Qu-NP as compared to quercetin suspension, which indicated the reduced dosing frequency. Efficacy in diabetic rats suggested that same dose of Qu-NP on every fifth day was sufficient to bring effect similar to daily dose of oral quercetin suspension, and the same effect was also observed for catalase and superoxide dismutase levels in pancreas and kidneys. Thus, the system offers an efficacious oral therapy with reduced dose and dosing frequency for treatment of diabetes and is hence patient compliant.

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Section: Introductionmentioning

confidence: 99%

“…However, pharmaceutically, quercetin is a challenging molecule to be delivered due to its poor solubility, low hydrophilicity (log P of 1.81), gastrointestinal instability, extensive first pass metabolism, and minimal absorption in gastrointestinal tract [2]. Quercetin belongs to BCS class II.…”

Section: Introductionmentioning

confidence: 99%

Development of quercetin nanoformulation and in vivo evaluation using streptozotocin induced diabetic rat model

Chitkara

Nikalaje

Mittal

et al. 2012

Drug Deliv. and Transl. Res.

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“…Oils and lipids are also important excipients employed in preclinical studies. Lecithin is a well-known stabilizer used in preclinical suspensions and emulsions and is known for its potential to improve oral absorption by increasing micellization of drugs in GIT (110,115). Many long-chain triglycerides and medium-chain triglycerides used as either the oil component of emulsions or as stabilizers are known to exert similar effects.…”

Section: Excipientsmentioning

confidence: 99%

Preclinical Formulations: Insight, Strategies, and Practical Considerations

et al. 2014

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Abstract. A lot of resources and efforts have been directed to synthesizing potentially useful new chemical entities (NCEs) by pharmaceutical scientists globally. Detailed physicochemical characterization of NCEs in an industrial setup begins almost simultaneously with preclinical testing. Most NCEs possess poor water solubility posing bioavailability issues during initial preclinical screening, sometimes resulting in dropping out of an NCE with promising therapeutic activity. Selection of right formulation approach for an NCE, based on its physicochemical properties, can aid in improving its solubility-related absorption and bioavailability issues. The review focuses on preclinical formulations stressing upon different preclinical formulation strategies and deciphers the understanding of formulation approaches that could be employed. It also provides detailed information related to a vast pool of excipients available today, which is of immense help in designing preclinical formulations. Few examples mentioned, throw light on key aspects of preclinical formulation development. The review will serve as an important guide for selecting the right strategy to improve bioavailability of NCEs for academic as well as industrial formulation scientists.

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“…This has been achieved through specialized uptake mechanisms, increased half-life (t 1/2 ), minimized toxicity, and increased ability of NPs to cross the physiological barriers such as the BBB. 9,10 To improve the oral bioavailability of QT, various attempts have been made by many researchers to formulate various drug delivery systems of current drug therapy, such as poly(D,L-lactide) (PLA) NPs, 7 solid lipid NPs, 8 lecithin-based novel cationic nanocarriers (LeciPlex), 11 chitosan NPs, 12 liposomes, 13 and poly(D,L-lactide-co-glycolide) (PLGA) NPs, 14 but all with limited effects. However, no detailed study has been reported on improving the brain permeability of the drug.…”

Section: Introductionmentioning

confidence: 99%

Poly(n-butylcyanoacrylate) nanoparticles for oral delivery of quercetin: preparation, characterization, and pharmacokinetics and biodistribution studies in Wistar rats

Bagad¹,

Khan²

2015

IJN

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Background Quercetin (QT) is a potential bioflavonol and antioxidant with poor bioavailability and very low distribution in the brain. A new oral delivery system comprising of poly(n-butylcyanoacrylate) nanoparticles (PBCA NPs) was introduced to improve the oral bioavailability of QT and to increase its distribution in the brain. Physicochemical characteristics, in vitro release, stability in simulated gastric fluid and intestinal fluids, and pharmacokinetics and biodistribution studies of QT-PBCA NPs coated with polysorbate-80 (P-80) were investigated. Objective This study aimed to investigate the physicochemical characteristics, in vitro release, stability in simulated gastric fluid and intestinal fluids, and pharmacokinetics and biodistribution studies of QT-PBCA NPs coated with polysorbate-80 (P-80). Results The results showed that QT-PBCA NPs and QT-PBCA NPs coated with P-80 (QT-PBCA+P-80) had mean particle sizes of 161.1±0.44 nm and 166.6±0.33 nm respectively, and appeared spherical in shape under transmission electron microscopy. The mean entrapment efficiency was 79.86%±0.45% for QT-PBCA NPs and 74.58%±1.44% for QT-PBCA+P-80. The in vitro release of QT-PBCA NPs and QT-PBCA+P-80 showed an initial burst release followed by a sustained release when compared to free QT. The relative bioavailability of QT-PBCA NPs and QT-PBCA+P-80 enhanced QT bioavailability by 2.38- and 4.93-fold respectively, when compared to free QT. The biodistribution study in rats showed that a higher concentration of QT was detected in the brain after the NPs were coated with P-80. Conclusion This study indicates that PBCA NPs coated with P-80 can be potential drug carriers for poorly water-soluble drugs. These NPs were observed to improve the drugs’ oral bioavailability and enhance their transport to the brain.

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Lecithin-Based Novel Cationic Nanocarriers (Leciplex) II: Improving Therapeutic Efficacy of Quercetin on Oral Administration

Cited by 98 publications

References 50 publications

Development of quercetin nanoformulation and in vivo evaluation using streptozotocin induced diabetic rat model

Development of quercetin nanoformulation and in vivo evaluation using streptozotocin induced diabetic rat model

Preclinical Formulations: Insight, Strategies, and Practical Considerations

Poly(n-butylcyanoacrylate) nanoparticles for oral delivery of quercetin: preparation, characterization, and pharmacokinetics and biodistribution studies in Wistar rats

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