Investigation of hydroxypropyl-β-cyclodextrin inclusion complexation of two poorly soluble model drugs and their taste-sensation - Effect of electrolytes, freeze-drying and incorporation into oral film formulations

Alopaeus, Julia Fredrika; Göbel, Anja; Breitkreutz, Jörg; Sande, Sverre Arne; Tho, Ingunn

doi:10.1016/j.jddst.2020.102245

Cited by 11 publications

(5 citation statements)

References 35 publications

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“…Further, the complexation efficiency 54 and drug–cyclodextrin molar ratio were calculated using eqs 5 and 6 ( 55 ) …”

Section: Methodsmentioning

confidence: 99%

“…In each dilution, 10 mg of AZM was added and kept stirring for 72 h. After this, the solution was filtered through a 0.45 μm membrane filter, and the amount of AZM was analyzed by a UV−visible spectrophotometer. 53 Further, the complexation efficiency 54 and drug−cyclodextrin molar ratio were calculated using eqs 5 and 6 55 = × − S K S complexation efficacy slope (1 slope) 0 0…”

Section: 7mentioning

confidence: 99%

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Cyclodextrin Derivative Enhances the Ophthalmic Delivery of Poorly Soluble Azithromycin

Thakur

Jain²,

Pant

et al. 2022

ACS Omega

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Azithromycin (AZM), a macrolide antibiotic used for the treatment of chlamydial conjunctivitis, is less effective for the treatment of this disease due to its poor bioavailability (38%). Various alternatives have been developed for improving the physicochemical properties (i.e., solubility) of the AZM without much success. To overcome the problems associated with AZM, an inclusion complex employing a modified cyclodextrin, i.e., sulfobutylether-β-cyclodextrin (SBE-β-CD), was prepared and characterized by phase solubility studies and PXRD techniques. The results portrayed the formation of an inclusion complex of AZM with SBE-β-CD in 1:2 molar stoichiometric ratios. This inclusion complex was later incorporated into a polymer matrix to prepare an in situ gel. Various combinations of Carbopol 934P and hydroxypropyl methylcellulose (HPMC K4M) polymers were used and evaluated by rheological and in vitro drug release studies. The optimized formulation (F4) containing Carbopol 934P (0.2% w/v) and HPMC K4M (0.2% w/v) was evaluated for clarity, pH, gelling capacity, drug content, rheological properties, in vitro drug release pattern, ocular irritation test, and antimicrobial efficacy. Finally, owing to the improved antimicrobial efficacy and increased residence time, the AZM:SBE-β-CD in situ gel was found to be a promising formulation for the efficient treatment of bacterial ocular disease.

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“…Further, the complexation efficiency 54 and drug–cyclodextrin molar ratio were calculated using eqs 5 and 6 ( 55 ) …”

Section: Methodsmentioning

confidence: 99%

Section: 7mentioning

confidence: 99%

Cyclodextrin Derivative Enhances the Ophthalmic Delivery of Poorly Soluble Azithromycin

Thakur

Jain²,

Pant

et al. 2022

ACS Omega

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“…In addition to the aforementioned dosage forms, other solid formulations have also been investigated, including extrudates from hot-melt extrusion [96][97][98], (mini-)tablets [99,100], orodispersible and mucoadhesive films [101,102], nanofibers from co-axial electrospinning [103,104], and SNEDDS-formulations [105].…”

Section: Other Solid Dosage Formsmentioning

confidence: 99%

Critical View on the Qualification of Electronic Tongues Regarding Their Performance in the Development of Peroral Drug Formulations with Bitter Ingredients

Steiner,

Meyer,

Immohr

et al. 2024

Pharmaceutics

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In this review, we aim to highlight the advantages, challenges, and limitations of electronic tongues (e-tongues) in pharmaceutical drug development. The authors, therefore, critically evaluated the performance of e-tongues regarding their qualification to assess peroral formulations containing bitter active pharmaceutical ingredients. A literature search using the keywords ‘electronic’, ‘tongue’, ‘bitter’, and ‘drug’ in a Web of Science search was therefore initially conducted. Reviewing the publications of the past decade, and further literature where necessary, allowed the authors to discuss whether and how e-tongues perform as expected and whether they have the potential to become a standard tool in drug development. Specifically highlighted are the expectations an e-tongue should meet. Further, a brief insight into the technologies of the utilized e-tongues is given. Reliable protocols were found that enable (i) the qualified performance of e-tongue instruments from an analytical perspective, (ii) proper taste-masking assessments, and (iii) under certain circumstances, the evaluation of bitterness.

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“…This CD has also been functionalized to improve their compatibility with polymers or water solubility. This is the case of hydroxypropyl-βCD (HPβCD), obtained through the functionalization of hydroxyl by hydroxypropyl groups, and commonly used for the complexation of poorly soluble drugs [21,22]. In general, both CDs presented acceptable K values, with the retention capacity of both tested CDs being very similar.…”

Section: Adsorption Capacity Of Voc Adsorbentsmentioning

confidence: 99%

Designing an Oxygen Scavenger Multilayer System Including Volatile Organic Compound (VOC) Adsorbents for Potential Use in Food Packaging

López-de-Dicastillo,

López-Carballo,

Vázquez

et al. 2023

Polymers

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Oxygen scavengers are valuable active packaging systems because several types of food deterioration processes are initiated by oxygen. Although the incorporation of oxygen scavenger agents into the polymeric matrices has been the trend in recent years, the release of volatile organic compounds (VOC) as a result of the reaction between oxygen and oxygen scavenger substances is an issue to take into account. This is the case of an oxygen scavenger based on a trans-polyoctenamer rubber (TOR). In this work, the design of an oxygen scavenger multilayer system was carried out considering the selection of appropriate adsorbents of VOCs to the proposed layer structure. Firstly, the retention of some representative organic compounds by several adsorbent substances, such as zeolites, silicas, cyclodextrins and polymers, was studied in order to select those with the best performances. A hydrophilic silica and an odor-adsorbing agent based on zinc ricinoleate were the selected adsorbing agents. The principal VOCs released from TOR-containing films were carefully identified, and their retention first by the pure adsorbents, and then by polyethylene incorporated with the selected compounds was quantified. Detected concentrations decreased by 10- to 100-fold, depending on the VOC.

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Investigation of hydroxypropyl-β-cyclodextrin inclusion complexation of two poorly soluble model drugs and their taste-sensation - Effect of electrolytes, freeze-drying and incorporation into oral film formulations

Cited by 11 publications

References 35 publications

Cyclodextrin Derivative Enhances the Ophthalmic Delivery of Poorly Soluble Azithromycin

Cyclodextrin Derivative Enhances the Ophthalmic Delivery of Poorly Soluble Azithromycin

Critical View on the Qualification of Electronic Tongues Regarding Their Performance in the Development of Peroral Drug Formulations with Bitter Ingredients

Designing an Oxygen Scavenger Multilayer System Including Volatile Organic Compound (VOC) Adsorbents for Potential Use in Food Packaging

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