Oral drug delivery research in Europe

Mrsny, Randall J.

doi:10.1016/j.jconrel.2012.01.017

Cited by 69 publications

(31 citation statements)

References 79 publications

(75 reference statements)

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“…Chewables were also specifically preferred over orodispersibles and multiparticulates 280 (Figure 3). From an anthropological perspective, this may be instinctive; the importance of chewing food is widely reiterated to children and mastication before swallowing is an innate mechanism for articles which enter the mouth (Mrsny, 2012). The natural tendency to chew was evidenced in the recent studies assessing acceptability and swallowing of mini-tablets, especially amongst those aged 2 to 3 years old (Thomson et al, 2009, Klingmann et al, 2013.…”

Section: Novel Dosage Formsmentioning

confidence: 99%

Age-appropriate and acceptable paediatric dosage forms: Insights into end-user perceptions, preferences and practices from the Children’s Acceptability of Oral Formulations (CALF) Study

Ranmal¹,

Cram

Tuleu³

2016

International Journal of Pharmaceutics

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A lack of evidence to guide the design of age-appropriate and acceptable dosage forms has been a longstanding knowledge gap in paediatric formulation development. The Children's Acceptability of Oral Formulations (CALF) study captured end-user perceptions and practices with a focus on solid oral dosage forms, namely tablets, capsules, chewables, orodispersibles, multiparticulates (administered with food) and mini-tablets (administered directly into the mouth). A rigorous development and testing phase produced age-adapted questionnaires as measurement tools with strong evidence of validity and reliability. Overall, 590 school children and adolescents, and 428 adult caregivers were surveyed across hospitals and various community settings. Attitudes towards dosage forms primarily differed based on age and prior use. Positive attitudes to tablets and capsules increased with age until around 14 years. Preference was seen for chewable and orodispersible preparations across ages, while multiparticulates were seemingly less favourable. Overall, 59.6% of school children reported willingness to take 10mm diameter tablets, although only 32.1% of caregivers perceived this size to be suitable. While not to be taken as prescriptive guidance, the results of this study provide some evidence towards rational dosage form design, as well as methodological approaches to help design tools for further evaluation of acceptability within paediatric studies.

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Section: Novel Dosage Formsmentioning

confidence: 99%

Age-appropriate and acceptable paediatric dosage forms: Insights into end-user perceptions, preferences and practices from the Children’s Acceptability of Oral Formulations (CALF) Study

Ranmal¹,

Cram

Tuleu³

2016

International Journal of Pharmaceutics

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“…Consequently, tremendous emphasis is being placed on engineering novel and effective oral drug delivery systems that significantly improve oral bioavailability [4, 5]. Amongst various approaches, the stability of formulations in the acidic environment of stomach can be improved by coating them with acid stable-pH sensitive polymers such as Eudragit ® (poly methacrylate) polymers [6]. Further, encapsulating drugs in a polymeric matrix such as in ethyl cellulose, alginate gels, and mucoadhesive patches can provide gastrointestinal stability against enzymatic degradation [7–10].…”

Section: Introductionmentioning

confidence: 99%

Role of nanoparticle size, shape and surface chemistry in oral drug delivery

Banerjee

Gogoi

et al. 2016

Journal of Controlled Release

589

314

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Nanoparticles find intriguing applications in oral drug delivery since they present a large surface area for interactions with the gastrointestinal tract and can be modified in various ways to address the barriers associated with oral delivery. The size, shape and surface chemistry of nanoparticles can greatly impact cellular uptake and efficacy of the treatment. However, the interplay between particle size, shape and surface chemistry has not been well investigated especially for oral drug delivery. To this end, we prepared sphere-, rod- and disc-shaped nanoparticles and conjugated them with targeting ligands to study the influence of size, shape and surface chemistry on their uptake and transport across intestinal cells. A triple co-culture model of intestinal cells was utilized to more closely mimic the intestinal epithelium. Results demonstrated higher cellular uptake of rod-shaped nanoparticles in the co-culture compared to spheres regardless of the presence of active targeting moieties. Transport of nanorods across the intestinal co-culture was also significantly higher than spheres. The findings indicate that nanoparticle-mediated oral drug delivery can be potentially improved with departure from spherical shape which has been traditionally utilized for the design of nanoparticles. We believe that understanding the role of nanoparticle geometry in intestinal uptake and transport will bring forth a paradigm shift in nanoparticle engineering for oral delivery and non-spherical nanoparticles should be further investigated and considered for oral delivery of therapeutic drugs and diagnostic materials.

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“…24,25 In addition to this, the drug can be easily applied and localized to the application site and can be removed directly by patients from there if necessary. 26,27 We prepared buccal tablet as a controlled and effective dosage form to let the drug release to oral saliva. The bioadhesive polymers were employed to increase the residence time of the drug in the oral cavity and the localization of the drug in a particular region.…”

Section: Introductionmentioning

confidence: 99%

Preparation, characterization, and evaluation of amphotericin B-loaded MPEG-PCL-g-PEI micelles for local treatment of oral <em>Candida albicans</em>

Zhou¹,

Zhang²,

Chen³

et al. 2017

IJN

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Fatal Candida albicans infections in the mucosal system can occur in association with immune-compromised diseases and dysbacteriosis. Currently, amphotericin B (AmB) is considered to be the most effective antibiotic in the treatment of C. albicans infections, but its clinical application is limited by side effects and poor bioavailability. In order to use AmB in the local treatment of oral C. albicans infections, AmB/MPEG-PCL-g-PEI (monomethoxy poly(ethylene glycol)-poly(epsilon-caprolactone)-graft-polyethylenimine, MPP) micelles were prepared. A series of characterizations were performed. The micelles allowed a sustained in vitro release in both normal oral conditions (pH 6.8) and C. albicans infection conditions (pH 5.8). Then, buccal tablets containing freeze-dried powder of AmB/MPP micelles were produced by direct compression process and evaluated as regards to weight variation, hardness, and friability. In vitro drug release of the buccal tablets was measured in both the United States Pharmacopeia dissolution apparatus and the dissolution rate test apparatus, which was previously designed for simulating in vivo conditions of the oral cavity. The buccal tablets could sustainably release within 8 h and meet the antifungal requirements. Regarding safety assessment of AmB/MPP micelles, in vivo histopathological data showed no irritation toward buccal mucosa of the rats in both optical microscopy and ultrastructure observation of the tissues. MTT experiment proved that AmB/MPP micelles reduced the cytotoxicity of AmB. The micelles delivered through the gastrointestinal route were also found to be non-systemic toxicity by liquid chromatography-mass spectrometry analysis. Furthermore, the antifungal action of AmB/MPP micelles was evaluated. Although AmB/MPP had no obvious improvement as compared to AmB alone in the antifungal effect on planktonic C. albicans , the micelles significantly enhanced the antifungal activity against the biofilm state of C. albicans . Thus, it was concluded that AmB/MPP micelles represent a promising novel drug delivery system for the local treatment of oral C. albicans infections.

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Oral drug delivery research in Europe

Cited by 69 publications

References 79 publications

Age-appropriate and acceptable paediatric dosage forms: Insights into end-user perceptions, preferences and practices from the Children’s Acceptability of Oral Formulations (CALF) Study

Age-appropriate and acceptable paediatric dosage forms: Insights into end-user perceptions, preferences and practices from the Children’s Acceptability of Oral Formulations (CALF) Study

Role of nanoparticle size, shape and surface chemistry in oral drug delivery

Preparation, characterization, and evaluation of amphotericin B-loaded MPEG-PCL-g-PEI micelles for local treatment of oral <em>Candida albicans</em>

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