Influence of chitosan nanoparticles as the absorption enhancers on salvianolic acid B In vitro and In vivo evaluation

Jin, Xin; Zhang, Shibing; Li, Shi-meng; Liang, Ke; Jia, Zeng-yong

doi:10.4103/0973-1296.176047

Cited by 20 publications

(4 citation statements)

References 33 publications

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“…Previous pharmacokinetic study has provided a hint that DO volatile oils mostly distributed and accumulated on rat intestine might affect the absorption of other drug ingredients 34 , but it has not been elucidated experimentally. In the present study, with the presence of DO volatile oils in QSYQ, the absorption of major ingredients in QSYQ, such as CS, ON, CG, PCA, TSL, RA, SAB, AIV were obviously enhanced compared to the absence of DO volatile oils in QSYQ-DO in isolated intestinal tract, especially for ON, CG, RA, SAB and AIV 35 – 38 , which have larger molecular weights and possess poor permeability across the intestinal epithelium.…”

Section: Discussionmentioning

confidence: 49%

A critical courier role of volatile oils from Dalbergia odorifera for cardiac protection in vivo by QiShenYiQi

Zhang

et al. 2017

Sci Rep

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Component-based Chinese medicine (CCM) is derived from traditional Chinese medicine but produced with modern pharmaceutical standard and clearer clinical indications. However, it still faces challenges of defining individual component contribution in the complex formula. Using QiShenYiQi (QSYQ) as a model CCM, we investigated the role of Dalbergia odorifera (DO), an herbal component, in preventing myocardial damage. We showed that in vitro, QSYQ exerted considerable protective activities on cardiomyocytes from H2O2-induced mitochondrial dysfunction with or without DO. However, in isolated rat hearts, myocardial protection by QSYQ was significantly weakened without DO. In everted gut sac model, DO significantly enhanced absorption of the major QSYQ ingredients in different regions of rat intestine. Finally, in in vivo mouse model of doxorubicin (DOX)-induced myocardial damage, only QSYQ, but not QiShenYiQi without DO (QSYQ-DO), exerted a full protection. Taken together, our results showed that instead of directly contributing to the myocardial protection, Dalbergia odorifera facilitates the major active ingredients absorption and increases their efficacy, eventually enhancing the in vivo potency of QSYQ. These findings may shed new lights on our understanding of the prescription compatibility theory, as well as the impacts of “courier herbs” in component-based Chinese medicine.

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Section: Discussionmentioning

confidence: 49%

A critical courier role of volatile oils from Dalbergia odorifera for cardiac protection in vivo by QiShenYiQi

Zhang

et al. 2017

Sci Rep

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“…This was further corroborated by a recent study that concluded that the absorption-enhancing effect of chitosan was drug-dependent, with acyclovir displaying unfavorable enhancement of absorption in the presence of chitosan [84]. On the other hand, there are studies that highlighted drugs that displayed an enhanced absorption with the aid of chitosan, and these include molecules such as buserelin, [ 14 C] mannitol, and dextran [79,85].…”

Section: Chitosanmentioning

confidence: 55%

“…The permeation rate and P app value of salvianolic acid B were found to be at a maximum when co-delivered with chitosan displaying a molecular weight of 100 kDa. However, with a decreasing molecular weight, the researchers also observed a decline in the permeation rate of salvianolic acid B [79]. It was proposed that the chitosan, which exhibits a positive surface charge, forms ionic interactions with the negatively charged glycocalyx groups, resulting in the reversibility of the opening tight junctions, which could improve the paracellular drug transport.…”

Section: Chitosanmentioning

confidence: 99%

Intestinal Absorption Study: Challenges and Absorption Enhancement Strategies in Improving Oral Drug Delivery

et al. 2022

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The oral route is the most common and practical means of drug administration, particularly from a patient’s perspective. However, the pharmacokinetic profile of oral drugs depends on the rate of drug absorption through the intestinal wall before entering the systemic circulation. However, the enteric epithelium represents one of the major limiting steps for drug absorption, due to the presence of efflux transporters on the intestinal membrane, mucous layer, enzymatic degradation, and the existence of tight junctions along the intestinal linings. These challenges are more noticeable for hydrophilic drugs, high molecular weight drugs, and drugs that are substrates of the efflux transporters. Another challenge faced by oral drug delivery is the presence of first-pass hepatic metabolism that can result in reduced drug bioavailability. Over the years, a wide range of compounds have been investigated for their permeation-enhancing effect in order to circumvent these challenges. There is also a growing interest in developing nanocarrier-based formulation strategies to enhance the drug absorption. Therefore, this review aims to provide an overview of the challenges faced by oral drug delivery and selected strategies to enhance the oral drug absorption, including the application of absorption enhancers and nanocarrier-based formulations based on in vitro, in vivo, and in situ studies.

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“…18 Indeed, these nano-sized carriers overcome intrinsic challenges encountered by drug molecules in gastrointestinal tract, and can also be modified to maintain the required drug release for therapeutic response. 19 Wide range of biocompatible polymers from synthetic and natural sources with specific properties have been explored for the formulation of nanoparticles intended for oral delivery. Among these, synthetic polymers are widely preferred as they possess good mechanical strength and can be modified to obtain well-defined release characteristics.…”

Section: Introductionmentioning

confidence: 99%

Poly(lactic acid-co-glycolic acid) Nanospheres Improved the Oral Delivery of Candesartan Cilexetil

Nair¹,

Al‐Dhubiab²,

Shah³

et al. 2017

IJPER

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Purpose: Certain physicochemical characteristics of Candesartan Cilexetil (CC) lead to incomplete oral absorption and poor clinical efficacy. This study assessed the prospect of the use of drug-embedded nanospheres to augment the oral bioavailability of CC. Methods: Baseline studies were conducted to measure the solubility of CC in the polymer. Drug encapsulated poly(lactic acid-co-glycolic acid) nanospheres were prepared by emulsion solvent evaporation method. Five different formulations (C1-C5) were prepared for the varying amount of CC (30-50 mg). Evaluation was carried out for nanospheres characters, drug dissolution and release kinetics. Pharmacokinetics parameters were evaluated in rat model. Results: Solubility of drug in polymer was ~20 mg/100 mg of poly(lactic acid-co-glycolic acid). Values of particle size (200-400 nm), zeta potential (~-25 to -27 mV) and polydispersity index (0.17 to 0.21) were optimal for oral absorption. Morphological studies suggest that the prepared nanospheres were spherical in shape with no aggregation. The nanospheres exhibited biphasic release of CC with an initial burst effect (~50% in 4 h), while it was low and incomplete (~54% in 14 h) with pure drug. Furthermore, drug release from nanospheres appeared to indicate a Korsmeyer-Peppas model (r2=0.981), and diffusion of the drug molecules was by anomalous transport (n=0.74). Greater and rapid absorption of CC was observed from the nanospheres with significantly higher C max (599.92 ± 139.36 ng/ml; P<0.0005) and AUC0 -∞ (~3 folds; P<0.0001) relative to the pure drug (control). Conclusion: These results suggested that CC loaded nanospheres seems to be a suitable alternative to improve the oral bioavailability and could be further assessed for clinical use.

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Influence of chitosan nanoparticles as the absorption enhancers on salvianolic acid B In vitro and In vivo evaluation

Cited by 20 publications

References 33 publications

A critical courier role of volatile oils from Dalbergia odorifera for cardiac protection in vivo by QiShenYiQi

A critical courier role of volatile oils from Dalbergia odorifera for cardiac protection in vivo by QiShenYiQi

Intestinal Absorption Study: Challenges and Absorption Enhancement Strategies in Improving Oral Drug Delivery

Poly(lactic acid-co-glycolic acid) Nanospheres Improved the Oral Delivery of Candesartan Cilexetil

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