Grinding as Solvent-Free Green Chemistry Approach for Cyclodextrin Inclusion Complex Preparation in the Solid State

Jug, Mario; Mura, Paola

doi:10.3390/pharmaceutics10040189

Cited by 59 publications

(36 citation statements)

References 97 publications

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“…In this study, the usefulness of a combined strategy, based on the drug interaction with a suitable CD, and the loading of the binary systems into NLC, has been evaluated in the development of an oral liquid formulation of HCT intended for pediatric use, able to assure safety, dosage accuracy, stability and therapeutic efficacy.Thus, the grinding procedure confirmed its efficiency for preparing cyclodextrin inclusion complex in the solid state [64].…”

Section: Discussionmentioning

confidence: 91%

Combined Approach of Cyclodextrin Complexationand Nanostructured Lipid Carriers for the Development of a Pediatric Liquid Oral Dosage Form of Hydrochlorothiazide

et al. 2018

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The development of specific and age-appropriate pediatric formulations is essential to assure that all children and their care-givers can easily access to safe and effective dosage forms. The need for developing specific pediatric medicinal products has been highlighted by the European Medicines Agency. The aim of this study was to investigate the effectiveness of combining the advantages of both cyclodextrin (CD) complexation and loading into nanostructured lipid carriers (NLC), to obtain a liquid oral pediatric formulation of hydrochlorothiazide (HCT), endowed with safety, dosage accuracy, good stability and therapeutic efficacy. Equimolar drug combinations as physical mixture (P.M.) or coground product (GR) with hydroxypropyl-β-cyclodextrin (HPβCD) or sulfobutylether-β-cyclodextrin (SBEβCD) were loaded into NLC, then characterized for particle size, homogeneity, Zeta potential, entrapment efficiency, gastric and storage stability. The presence of HPβCD allowed higher entrapment efficacy than NLC loaded with the plain drug, and enabled, in the case of GR systems a complete and sustained drug release, attributable to the wetting and solubilising properties of HPβCD toward HCT. In vivo studies on rats proved the superior therapeutic effectiveness of HCT-in HPβCD-in NLC formulations compared to the corresponding free HCT-loaded NLC, thus confirming the successfulness of the proposed approach in the development of an efficacious liquid oral formulation of the drug.

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Section: Discussionmentioning

confidence: 91%

Combined Approach of Cyclodextrin Complexationand Nanostructured Lipid Carriers for the Development of a Pediatric Liquid Oral Dosage Form of Hydrochlorothiazide

et al. 2018

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“…Solid inclusion complexes of rutin with β-CD and HP-β-CD were prepared by four different methods, including formation in the semisolid state (Methods 1 and 2), formation in the solid state (Method 3) and formation in solution (Method 4) (Jug and Mura, 2018). All samples were initially analysed by PXRD, DSC and FTIR and, based on the results showing the greatest interactions between the components (by DSC and FTIR) as well as the largest degree of solid-state changes (by PXRD), the most appropriate method of formation was chosen.…”

Section: Production and Solid-state Characterisation Of The Rutin Sammentioning

confidence: 99%

Mechanochemical activation with cyclodextrins followed by compaction as an effective approach to improving dissolution of rutin

Paczkowska

McDonagh

Bialek

et al. 2020

International Journal of Pharmaceutics

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Rutin is one of the most important flavonoids with poor bioavailability. This work aimed at addressing the issue of poor biopharmaceutical performance of rutin by applying a combination of complexation with secondary processing into tablets. Mechanical activation was the most suitable method of rutin complex formation with (2-hydroxypropyl)-β-cyclodextrin (HP-β-CD), while the β-cyclodextrin (β-CD) complex successfully formed by kneading with an ethanol/water mixture. Complexation was confirmed by thermal analysis, powder X-ray diffraction and vibrational spectroscopy. Dynamic vapour sorption showed that stability of powders at high humidity conditions was satisfactory, however, the β-CD complex retained around 8% of moisture. The complexes were compacted with or without tricalcium phosphate (TRI-CAFOS) filler at a range of compression pressures (19-113 MPa). The best tabletability was determined for rutin/HP-β-CD, compressibility for the TRI-CAFOS blends with complexes and compactibility for the rutin/HP-β-CD+TRI-CAFOS mix. Dissolution studies showed quicker and more complete dissolution (pH 1.2) of rutin/HP-β-CD tablets, however the compacts comprising the filler were superior than pure complexes. The tablets manufactured in this study appear to be promising delivery systems of rutin and it is recommended to combine rutin/HP-β-CD with TRI-CAFOS and compact at 38-76 MPa.

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“…This phenomenon can be predicted because of the intermolecular hydrogen bonds between atenolol and β-cyclodextrin. This condition caused by the restriction of atenolol packing in cyclodextrin cavity 27 . Moreover, in inclusion complexes that had been prepared by kneading and solvent evaporation method, two functional groups (-CO-NH) had been bounded by functional OH groups of β-cyclodextrin through hydrogen bonding 27 .…”

Section: Fig 1: Infrared Spectrum Of Inclusion Complexes Of Atenololmentioning

confidence: 99%

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Rani¹,

Parfati²,

stephanie³

2020

IJPSR

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Atenolol is a hypertension drug that has a low solubility characteristic in water and gastric fluid. The rate of absorption of the drug with poor solubility characteristics is determined by the dissolution process. In this study, an attempt has been conducted to increase the dissolution of atenolol by increasing its solubility. The solubility of atenolol has been enhanced by the inclusion complex using βcyclodextrin made by several methods (physical mixing, kneading, and solvent evaporation). Evaluation and characterization of atenolol-βcyclodextrin inclusion complex consist of drug content, dissolution test, Fourier Transformed Infrared analysis (FT-IR), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) and Scanning Electron Microscope (SEM). The results of the drug content analysis, dissolution test, and characterization showed that atenolol-β-cyclodextrin inclusion complex, which has been made by the solvent evaporation method was the best approach. Therefore, a solvent evaporation method was chosen to formulate orally disintegrating tablets of atenolol-β-cyclodextrin using direct compression technique. Orally disintegrating tablets of atenolol-βcyclodextrin were prepared using crospovidone as disintegrant. The results of pre-compression test and the post-compression test revealed that orally disintegrating tablets of atenolol-β-cyclodextrin inclusion complex disintegrate within 8.17 ± 0.41 sec. In-vitro dispersion time in simulated saliva was found to be 45.33 ± 0.58 sec and the percentage of atenolol dissolved from this formula was 92.22% in 30 min. Hence, this formula shows good physicochemical characteristics and fulfill pharmaceutical quality requirements of orally disintegrating tablet.

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Grinding as Solvent-Free Green Chemistry Approach for Cyclodextrin Inclusion Complex Preparation in the Solid State

Cited by 59 publications

References 97 publications

Combined Approach of Cyclodextrin Complexationand Nanostructured Lipid Carriers for the Development of a Pediatric Liquid Oral Dosage Form of Hydrochlorothiazide

Combined Approach of Cyclodextrin Complexationand Nanostructured Lipid Carriers for the Development of a Pediatric Liquid Oral Dosage Form of Hydrochlorothiazide

Mechanochemical activation with cyclodextrins followed by compaction as an effective approach to improving dissolution of rutin

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