Cyclodextrin complexation: influence on the solubility, stability, and cytotoxicity of camptothecin, an antineoplastic agent

Kang, Jichao; Kumar, Vijay; Yang, Dong; Chowdhury, Priyanka; Hohl, Raymond J.

doi:10.1016/s0928-0987(01)00214-7

Cited by 125 publications

(91 citation statements)

References 23 publications

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“…Moreover, similar results of increasing stability from complexation and/or inclusion affinity with CDs were obtained with astaxanthin, warfarin, camptothecin, and taxol (Chen et al, 2007;Dordunoo and Burt, 1996;Kang et al, 2002;Zingone and Rubessa, 2005).…”

Section: Effect Of Cyclodextrins On Artemisinin Stabilitysupporting

confidence: 69%

Effect of cyclodextrins on artemisinin stability and <i>in vitro</i> dissolution

Zimé-Diawara¹,

Gbaguidi²,

Semdé³

et al. 2014

Int. J. Bio. Chem. Sci

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Artemisinin is extracted from the Asian plant Artemisia annua L. It has been proven to be, with its derivatives, the molecules that have shown so far the most powerful activity on malaria, even in its complicated forms and resistance cases. To resolve the problem of low aqueous solubility of this molecule, the use of cyclodextrins (CDs) was envisaged and gave good results in this topic. However, the impact on its stability and in vitro dissolution, important parameters for drug formulation and evaluation, was not evaluated. In this study, stability in accelerated degradation conditions and in vitro dissolution analysis of artemisinin were performed in comparison with complexes of artemisinin and cyclodextrins. The findings of this work allowed us to suggest that CDs improve the stability of artemisinin, especially when it's in aqueous solution. We also demonstrated the beneficial impact of cyclodextrins on the in vitro dissolution of artemisinin from capsules prepared with rough extracts of A. annua.

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Section: Effect Of Cyclodextrins On Artemisinin Stabilitysupporting

confidence: 69%

Effect of cyclodextrins on artemisinin stability and <i>in vitro</i> dissolution

Zimé-Diawara¹,

Gbaguidi²,

Semdé³

et al. 2014

Int. J. Bio. Chem. Sci

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“…CPT is an antineoplastic agent that exerts its anti-tumor effect by the inhibition of the nuclear enzyme topo isomerase I [76]. Although CPT shows a broad spectrum of activity towards many cancers it has yet to be used in vivo due to its poor solubility and rapid hydrolysis to a ring-open carboxylate form with lower pharmacological activity [61].…”

Section: Resultsmentioning

confidence: 99%

Controlled Drug Delivery From Composites of Nanostructured Porous Silicon and Poly( L -Lactide)

et al. 2012

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Aims: Porous silicon (pSi) and poly(L-lactide) (PLLA) both display good biocompatibility and tunable degradation behavior, suggesting that composites of both materials are suitable candidates as biomaterials for localized drug delivery into the human body. The combination of a pliable and soft polymeric material with a hard inorganic porous material of high drug loading capacity may engender improved control over degradation and drug release profiles and be beneficial for the preparation of advanced drug delivery devices and biodegradable implants or scaffolds. Materials & methods: In this work, three different pSi and PLLA composite formats were prepared. The first format involved grafting PLLA from pSi films via surface-initiated ring-opening polymerization (pSi–PLLA [grafted]). The second format involved spin coating a PLLA solution onto oxidized pSi films (pSi–PLLA [spin-coated]) and the third format consisted of a melt-cast PLLA monolith containing dispersed pSi microparticles (pSi–PLLA [monoliths]). The surface characterization of these composites was performed via infrared spectroscopy, scanning electron microscopy, atomic force microscopy and water contact angle measurements. The composite materials were loaded with a model cytotoxic drug, camptothecin (CPT). Drug release from the composites was monitored via fluorimetry and the release profiles of CPT showed distinct characteristics for each of the composites studied. Results: In some cases, controlled CPT release was observed for more than 5 days. The PLLA spin coat on pSi and the PLLA monolith containing pSi microparticles both released a CPT payload in accordance with the Higuchi and Ritger–Peppas release models. Composite materials were also brought into contact with human lens epithelial cells to determine the extent of cytotoxicity. Conclusion: We observed that all the CPT containing materials were highly efficient at releasing bioactive CPT, based on the cytotoxicity data. Original submitted 16 December 2010; Revised submitted 29 September 2011; Published online 6 March 2012

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“…The elimination half life of CPT is 58.7 mins. 3 The dose of the CPT is 200 mg/day for individual weighing 70 kg. 4 Since the elimination half life is short and its solubility is quite low, enhanced dissolution and sustained/controlled release characteristics are needed for CPT for better therapeutic efficacy.…”

Section: Introductionmentioning

confidence: 99%

“…Different approaches have been utilized to alleviate solubility and stability issues of CPT. [3][4][5] Most of the research works were focused on the particulate delivery of the CPT and its analogues especially as liposomes and nanoparticles. [6][7][8][9][10][11] Very few reports were published on the delivery of CPT and its analogues by oral matrix tablet technology.…”

Section: Introductionmentioning

confidence: 99%

“…Literature survey revealed that the solubility and stability of CPT was successfully enhanced by inclusion complexation with cyclodextrins. [3][4][5] Hence, in this investigation solubilizing excipients like cyclodextrins (β-cyclodextrin and hydroxyl propyl-β-cyclodextrin) were included in the formulations and their effect on the CPT release was studied in order to achieve therapeutically effective levels of CPT CR from matrix tablets.…”

Section: Introductionmentioning

confidence: 99%

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Studies on Development of Controlled Release Matrix Tablets of Camptothecin-An Anticancer Drug

Nalluri¹,

Devineni²,

Male³

et al. 2015

IJPER

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Objectives: The present investigation was carried out with an objective of formulating prototype controlled release (CR) matrix tablets of Camptothecin (CPT), an anti-cancer drug. Experimental: pH solubility profile studies of CPT and solubility of CPT in different surfactants were carried out. Controlled release tablets were prepared by direct compression method using hydroxyl propylmethyl cellulose (HPMC LVCR and HPMC K4M) as release retardants. The effect of different grades of microcrystalline cellulose (MCC) like Avicel PH 101 and Avicel PH 105 and solubilizing agents like cyclodextrins were included in the formulations and their effect on CPT release from tablets were studied. Results and Discussion: Solubility studies were conducted in order to select suitable dissolution medium for CPT. Based on the solubility studies, 0.1N HCl with 3% w/v SLS (pH1.2) was selected as dissolution medium. The FTIR and DSC results indicated that there was no in situ interaction between CPT and the selected excipients in the formualtions. Formulations containing 20% w/w of hydroxypropyl-β-cyclodextrin with Avicel PH105 as filler and HPMC k4M as release retardant gave superior CPT release of 98.40 ± 1.02% at the end of 12 h and fulfilled the regulatory requirements. The Higuchi square root model showed higher correlation coefficient values (0.949-0.990) indicating diffusion was the release mechanism for CPT from tablets. Conclusion: CPT can be formulated in to CR matrix tablets using HPMC K4M as release retardant and MCC as filler for better therapeutic efficacy.

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Cyclodextrin complexation: influence on the solubility, stability, and cytotoxicity of camptothecin, an antineoplastic agent

Cited by 125 publications

References 23 publications

Effect of cyclodextrins on artemisinin stability and <i>in vitro</i> dissolution

Effect of cyclodextrins on artemisinin stability and <i>in vitro</i> dissolution

Controlled Drug Delivery From Composites of Nanostructured Porous Silicon and Poly( L -Lactide)

Studies on Development of Controlled Release Matrix Tablets of Camptothecin-An Anticancer Drug

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