Solubilisation of drugs in worm-like micelles of block copolymers of ethylene oxide and 1,2-butylene oxide in aqueous solution

Zhou, Zhengyuan; Chaibundit, Chiraphon; D’Emanuele, Antony; Lennon, Kieran; Attwood, David; Booth, Colin

doi:10.1016/j.ijpharm.2007.10.028

Cited by 24 publications

(17 citation statements)

References 22 publications

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“…The conversion from the crystalline II form to the crystalline I phase was encouraged by two excipients, ECOSURF SA-7 and HO-(BO) 29 -(EO) 90 -H. Only two excipients tested appeared to be capable of keeping probucol mostly in its amorphous state during the 21-day aging test, octadecyl-O-(BO) 4 -(EO) 10 -H and octadecyl-O-(BO) 4 -(EO) 20 -H. This result is in agreement with the published observation of drug solubilization by diblock EO–BO copolymers. 54,55 In our previous study, several alkoxy-BO/EO excipients enabled a substantial increase in aqueous drug solubility. 42 The mixture of probucol with myrtenyl-O-(BO) 8 -(EO) 24 -H showed an almost 8000-fold increase in probucol solubility, and this solubility increase was retained even after aging for four months at 40 °C and 75% relative humidity.…”

Section: Resultsmentioning

confidence: 91%

High-Throughput Raman Spectroscopy Screening of Excipients for the Stabilization of Amorphous Drugs

et al. 2015

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Low aqueous solubility of active pharmaceutical ingredients (APIs) is an enduring problem in pharmaceutical development, and it is becoming increasingly prevalent among new drug candidates. It is estimated that about 40% of drugs in the development pipeline and approximately 60% of the drugs coming directly from discovery suffer from poor aqueous solubility and slow dissolution, thereby reducing their bioavailability and efficacy and thus preventing their commercialization. It is well known that utilizing the amorphous form of a drug can be a useful approach to improve the dissolution rate and solubility of poorly water-soluble APIs. Amorphous compounds are thermodynamically unstable, but they can be stabilized by combining them with a carrier polymer (excipient) to form a solid dispersion. High-throughput Raman spectroscopy was used in this study to identify excipients that promote formation and stabilization of the amorphous drug form in solid dispersions. Four model APIs were used as poorly soluble drug candidates: ketoprofen, danazol, griseofulvin, and probucol. The Raman signals of excipients were generally negligible, and therefore Raman bands from the drugs were used with minimal spectral pre-processing. By comparing Raman spectra collected from the APIs in the crystalline and molten state, appropriate spectral features and regions were identified for the development of semi-quantitative methods to determine the amorphous content for each API. It is demonstrated that methods based on peak intensity ratio, peak width, peak distance, and classical least squares can all be effective methods for the screening of excipients. Interesting excipient-dependent phase transformation behavior was also observed for probucol.

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Section: Resultsmentioning

confidence: 91%

High-Throughput Raman Spectroscopy Screening of Excipients for the Stabilization of Amorphous Drugs

et al. 2015

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“…Griseofulvin and spironolactone were solubilized to a greater extent than the more water-soluble drug, carbamazepine. The change in shape was responsible for greater solubilization of the drugs [254]. Contrarily, the process of solubilization can also influence micelle geometry.…”

Section: F127mentioning

confidence: 97%

Polymeric micelles: authoritative aspects for drug delivery

Kulthe

Choudhari

Inamdar

et al. 2012

Designed Monomers and Polymers

193

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“…These techniques allow synthesizing polymers of well‐controlled length and low polydispersity, and can be employed to finely tune the hydrophilic and hydrophobic block length in amphiphilic block copolymers (ABC). By using selective solvents, temperature or other stimuli it is then possible to control the self‐assembly of ABC and obtain a plethora of nanostructures ranging from spherical and worm‐like micelles to vesicles . Poly( N , N ‐dimethylacrylamide)‐ b ‐polystyrene (PDMA‐ b ‐PS) is one of those polymers, that already demonstrated the capability to form core–corona NP and hierarchical granular NP …”

Section: Introductionmentioning

confidence: 99%

Investigation of Functionalized Poly(N,N‐dimethylacrylamide)‐block‐polystyrene Nanoparticles As Novel Drug Delivery System to Overcome the Blood–Brain Barrier In Vitro

Gregori

Bertani

Cazzaniga

et al. 2015

Macromolecular Bioscience

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In the search of new drug delivery carriers for the brain, self-assembled nanoparticles (NP) were prepared from poly(N,N-dimethylacrylamide)-block-polystyrene polymer. NP displayed biocompatibility on cultured endothelial cells, macrophages and differentiated SH-SY5Y neuronal-like cells. The surface-functionalization of NP with a modified fragment of human Apolipoprotein E (mApoE) enhanced the uptake of NP by cultured human brain capillary endothelial cells, as assessed by confocal microscopy, and their permeability through a Transwell Blood Brain Barrier model made with the same cells, as assessed by fluorescence. Finally, mApoE-NP embedding doxorubicin displayed an enhanced release of drug at low pH, suggesting the potential use of these NP for the treatment of brain tumors.

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Solubilisation of drugs in worm-like micelles of block copolymers of ethylene oxide and 1,2-butylene oxide in aqueous solution

Cited by 24 publications

References 22 publications

High-Throughput Raman Spectroscopy Screening of Excipients for the Stabilization of Amorphous Drugs

High-Throughput Raman Spectroscopy Screening of Excipients for the Stabilization of Amorphous Drugs

Polymeric micelles: authoritative aspects for drug delivery

Investigation of Functionalized Poly(N,N‐dimethylacrylamide)‐block‐polystyrene Nanoparticles As Novel Drug Delivery System to Overcome the Blood–Brain Barrier In Vitro

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