Preparation of inclusion complex of apigenin-hydroxypropyl-β-cyclodextrin by using supercritical antisolvent process for dissolution and bioavailability enhancement

Huang, Yannian; Zu, Yuangang; Zhao, Xiuhua; Wu, Mingfang; Feng, Zi‐Qi; Deng, Yiping; Zu, Chang; Wang, Lingling

doi:10.1016/j.ijpharm.2016.08.007

Cited by 79 publications

(48 citation statements)

References 27 publications

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“…Pharmacokinetic analysis indicated that apigenin‐loaded soybean oil‐Tween 80 emulsion showcased greater bioavailability as compared with orally delivered apigenin suspensions . The solubility of inclusion complex of apigenin‐hydroxypropyl‐β‐cyclodextrin was approximately 152.43 times higher as compared with simple apigenin . Dissolution rates of AP‐HP‐β‐CD inclusion complexes were around 7.60 times higher as compared with simple apigenin …”

Section: Bioavailability Of Apigeninmentioning

confidence: 99%

Apigenin as an effective anticancer natural product: Spotlight on TRAIL, WNT/β‐catenin, JAK‐STAT pathways, and microRNAs

Özbey

Attar

Romero

et al. 2018

J of Cellular Biochemistry

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Wealth of information gleaned from decades of high‐impact research work; scientists have disentangled the complicated web of versatile regulators that underlie cancer development and progression. Use of structural biology approaches and functional genomics have helped us to gain new insights into complex nature of cancer, and it is now clear that genetic/epigenetic mutations, overexpression of oncogenes, inactivation of tumor suppressors, loss of apoptosis, and versatility of protein binding partners have contributory roles in carcinogenesis and metastatic spread. It is becoming progressively more understandable that reprogramming of gene expression during and nontranscriptional changes during cancer development and progression are initiated and controlled by deregulated signal transduction cascades, all of which collectively create an incalculable complexity. Data obtained through preclinical and clinical trials revealed that alterations in the targeted oncogenes and other downstream, and parallel pathways played a central role in the development of resistance against different therapeutics. Phytochemicals have regained limelight, and different natural products are currently being tested for efficacy in preclinical studies. Apigenin, a plant‐derived flavonoid has considerable pharmacological value and is reportedly involved in the regulation of different signaling cascades. In this review, we have attempted to summarize rapidly evolving understanding of molecular biologists and pharmacologists about the potential of apigenin in the regulation of deregulated signaling pathways in different cancers. We have emphasized on the regulation of WNT/β‐catenin and janus kinase/signal transducers and activators of transcription (JAK‐STAT) pathways. We also comprehensively discuss how apigenin restored apoptosis in tumor necrosis factor‐related apoptosis‐inducing ligand (TRAIL)‐resistant cancers. The review also gives a snapshot of microRNAs (miRNAs) that regulate wide‐ranging biological processes, and it is now clear that each miRNA can control hundreds of gene targets. Apigenin was noted to upregulate miR‐520b and miR‐101 in different cancers to inhibit tumor growth. Moreover, apigenin‐induced apoptotic rate was significantly higher when used in combination with miR‐423‐5p inhibitors or miR‐138 mimics. Better comprehension of linear and integrated signaling pathways will be helpful in effective therapeutic targeting of deregulated signaling pathways to inhibit/prevent cancer.

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Section: Bioavailability Of Apigeninmentioning

confidence: 99%

Apigenin as an effective anticancer natural product: Spotlight on TRAIL, WNT/β‐catenin, JAK‐STAT pathways, and microRNAs

Özbey

Attar

Romero

et al. 2018

J of Cellular Biochemistry

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“…Due to this characteristics nature, CDs have attained a great interest as a solubilising candidate and has overcome the biopharmaceutical deficiencies of various drugs in the recent years. 14,[17][18][19] CDs are widely soluble in some polar, aprotic solvents, but insoluble in most organic solvents. 20 Although, CDs exhibit higher solubility in some of the organic solvents than in water, inclusion complexes do not take place in non-aqueous solvents because of the increased affinity of guest molecule for the solvent compared to its affinity for water.…”

Section: Structure Of Cdsmentioning

confidence: 99%

“…The application of hydroxypropyl-β-cyclodextrin showed improved solubility of Altretamine by complexation approach. 38 Huang et al 19 prepared inclusion complex of apigeninhydroxypropyl-β-cyclodextrin by using supercritical antisolvent process using N,N-dimethyl formamide as solvent and carbon dioxide as antisolvent for the enhancement of dissolution and bioavailability. The mole ratio of apigenin and hydroxypropyl-β-cyclodextrin was kept 1:1.…”

Section: Figure 1 Depicts the Guest-host Inclusion Complexes Formationmentioning

confidence: 99%

“…Hence, the results showed that the prepared apigenin-hydroxypropyl-β-cyclodextrin inclusion complex serves as a potential approach for new oral therapeutic agent formulation. 19 Miyake et al 39 improved solubility, dissolution rate, and oral bioavailability of rutin by complexation with 2-hydroxypropyl-β-cyclodextrin. The in vivo absorption study revealed that hydroxypropyl-β-cyclodextrin increased the oral bioavailability of rutin from the gastrointestinal tracts due to increase in solubility, faster dissolution rate, and gastrointestinal stability.…”

Section: Figure 1 Depicts the Guest-host Inclusion Complexes Formationmentioning

confidence: 99%

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Cyclodextrin: A Promising Candidate in Enhancing Oral Bioavailability of poorly Water Soluble Drugs

Maheriya¹

2017

MOJBB

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Most of the drugs administered through oral route have poor aqueous solubility and dissolution rate. Cyclodextrin and its derivates represent as pharmaceutical adjuvants to overcome this challenges and helps in development of stable formulation with enhanced bioavailability. Cyclodextrins are unique structure with versatile physicochemical properties which aids the pharmaceutical scientists to overcome drug delivery challenges for poorly aqueous soluble drugs. Cyclodextrin and its derivates are widely useful as solubilizers, assisting in preparation of various dosage forms such as liquid oral, solid, and parenteral preparations. Cyclodextrins interacts with appropriately sized guest molecules to form inclusion complex and enhance the aqueous solubility, physical chemical stability, and bioavailability of drugs. Through the various reported literatures, the review highlights the concept of cyclodextrin and its derivatives in enhancing solubility and bioavailability of poorly aqueous soluble drugs.

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“…In order to improve the solubility, stability and bio-availability of ATM, we prepared ATM-2-HP-β-CD inclusion complex. 22 The ATM-2-HP-β-CD inclusion complex obtained by Solution mixing method under the optimum conditions was characterized using DSC, FTIR, and HPLC chromatography analyses. In addition, the appearance, melting point, dissolution, solubility characteristics and pharmacokinetic parameter of the ATM-2-HP-β-CD inclusion complex were also researched in this study.…”

mentioning

confidence: 99%

Inclusion Complex of Artemether with 2-Hydroxypropyl -β-Cyclodextrin for the Treatment of Malaria: Preparation, Characterization and Evaluation

Hao¹,

Chen²,

Tian³

et al. 2017

MOJBB

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Abbreviations: ATM, artemether; DSC, differential scanning calorimetry; FT-IR, fourier transform infrared spectroscopy; AUC, area under curve; MRT, mass rapid transit; CDs, cyclodextrins; HPLC, high performance liquid chromatography; LE, load efficiency IntroductionMalaria has a serious influence on human beings especially on that in tropical and subtropical countries. It is reported that there are approximately 300-500 million in clinical and 1.5-2.7 million in death every year. Among them, Plasmodium falciparum is the main protozoon for fatal cases. 1 With the widespread drug resistance limited by older therapies dominated by quinine, standard therapy for malaria is now artemisinin-based chemotherapy which is genuine and of high quality. 2 Artemether, [3R-(3R,5aS,6S,8aS,9R ,10R,12S,12aR)]- 6,-1,2-benzodioxepin, 3 is one of the lipidsoluble derivative of artemisinin, which has proved to be efficient against malaria especially for malignant malaria. 4 The structural formula is shown in Figure 1A. ATM disturbs the mitochondrial function, influence ultrastructure, and block the nutritional intake of Plasmodium falciparum, making them to lose cytoplasm and nutrients and cannot get replenish and soon died. 5,6 ATM belongs to BCS IV drug with poorly soluble and poorly permeable peculiarity. 7 ATM is only available as a pre-mixed oilbased solution for intramuscular injection. And there is evidence that the intramuscular injection may not be absorbed absolutely and can cause terrible pain to patient. 8,9 The novel delivery system such as liposome 10 and nanostructured lipid 11 of ATM did not achieve its aim of improving anti-malarial therapeutic efficiency. In addition, its poor bioavailability and rapid clearance from the body limits its exploitation and application in clinical study. From the analysis mentioned above, we can realize the importance of improving its solubility and bioavailability. Several formulation approach could be used to improving the solubility along with bio-availability of insoluble drugs. 12 Until now, different formulations are reported such as Solid Dispersion System, 7 nanoparticle, 13 inclusion complex. 1 Among them, inclusion complex is widely elected due to their mass production achieved easily.As a kind of functional excipients, cyclodextrins (CDs) have been used extensively in pharmaceutical formulations to improve the bio- AbstractArtemether (ATM) is being evaluated for use in Malaria at present. However, its poor solubility in water limits its exploitation and application in clinical. The purpose of this work is to develop inclusion complex of ATM with 2-hydroxypropyl-β-cyclodextrin (ATM-2-HP-β-CD inclusion complex) which have the ability to improve the solubility and oral bioavailability of ATM. The ATM-2-HP-β-CD inclusion complex was prepared by Solution mixing method at the mole ratio of 1:36 (ATM: HP-2-β-CD). The average drug entrapment efficiency and loading capacity were 97.66±1.22% and 2.64±0.03%, respectively. The formation of ATM-2-HP-β-CD inclusion complex was verified by ...

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Preparation of inclusion complex of apigenin-hydroxypropyl-β-cyclodextrin by using supercritical antisolvent process for dissolution and bioavailability enhancement

Cited by 79 publications

References 27 publications

Apigenin as an effective anticancer natural product: Spotlight on TRAIL, WNT/β‐catenin, JAK‐STAT pathways, and microRNAs

Apigenin as an effective anticancer natural product: Spotlight on TRAIL, WNT/β‐catenin, JAK‐STAT pathways, and microRNAs

Cyclodextrin: A Promising Candidate in Enhancing Oral Bioavailability of poorly Water Soluble Drugs

Inclusion Complex of Artemether with 2-Hydroxypropyl -β-Cyclodextrin for the Treatment of Malaria: Preparation, Characterization and Evaluation

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