Effect of casting solvent, film-forming agent and solubilizer on orodispersible films of a polymorphic poorly soluble drug: an<i>in vitro</i>/<i>in silico</i>study

El-Bary, A. Abd; Sharabi, Ibrahim Al; Haza'a, Balqees Saeed

doi:10.1080/03639045.2019.1656733

Cited by 17 publications

(15 citation statements)

References 81 publications

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“…The presence of moisture imparts flexibility and elasticity to the films so prevents their dryness and brittleness as water has a plasticizing effect. Moisture uptake indicates the hygroscopicity of the film and the necessity of specific packaging and storage conditions (El-Bary et al, 2019 ). Dry conditions lead to loss of water from polymeric films while they absorb moisture in conditions of RH above 60% (Fahmy & Badr-Eldin, 2014 ).…”

Section: Resultsmentioning

confidence: 99%

Formulation, characterization, optimization, and in-vivo performance of febuxostat self-nano-emulsifying system loaded sublingual films

et al. 2021

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Febuxostat (FXS) is a potent antigout drug with poor water solubility and relative high first-pass effect leading to moderate oral bioavailability (<49%). This study aimed to increase FXS solubility and bioavailability by optimizing sublingual fast-dissolving films (SFs) containing a selected FXS self-nanoemulsifying system (s-SNES) previously prepared by our team. The s-SNES was loaded into SFs by solvent casting technique. A full factorial design (3 2 ) was applied to study the effects of polymer and plasticizer types on mechanical characteristics and the dissolution profile of FXS from the SFs. Numerical optimization was performed to select the SF having highest desirability according to predetermined characteristics. The optimized SF (O-SF) contained 1 g of s-SNES, polyvinylpyrrolidone K30 (6%w/v), polyethylene glycol 300 (20%w/w of polymer wt.), and Avicel PH101 (0.5%w/v). O-SF showed good permeation of FXS through sheep sublingual tissue. Storage of O-SF for three months showed no significant change in the FXS dissolution profile. In-vivo performance of O-SF in rabbits was compared to that of oral marketed tablets (Staturic V R 80 mg). A cross-over design was applied and pharmacokinetic parameters were calculated after ensuring absence of sequence effect. Statistical analysis revealed better performance for O-SF with significantly higher C max , AUC 0-24 , AUC 0-1 , apparent t 1/2 together with lower t max , and apparent k el than marketed tablets. Relative bioavailability of O-SF compared to the marketed tablet was found to be 240.6%. This confirms the achievement of the study aims of improving dissolution rate and bioavailability of FXS using a patient-wise convenient formula.

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Section: Resultsmentioning

confidence: 99%

Formulation, characterization, optimization, and in-vivo performance of febuxostat self-nano-emulsifying system loaded sublingual films

et al. 2021

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“…As an example, sodium alginate has been used as an orodispersible film-forming polymer to provide mucoadhesive properties of the films or to increased drug loading or both. These applications are mostly accomplished with the sodium alginate alone to load poorly soluble drugs in ODF [22], or in combination with other polymers such as polyvinyl alcohol, chitosan, Carbopol 974P, and sodium carboxymethyl cellulose [22,23,50]. Various ODF formulations applying the uniqueness of alginates to provide different functions in the dosage form are exemplified in (Table 1).…”

Section: Applications Of Alginates In Orodispersible Dosage Formsmentioning

confidence: 99%

Applications of Alginates in the Design and Preparation of Orodispersible Dosage Forms

Khalid¹,

Selmin²

2022

Properties and Applications of Alginates

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Orodispersible dosage forms are attractive and innovative drug delivery systems that can fulfill individual patient needs, especially in children, elderly and among dysphagic patients. Indeed, they rapidly disperse in the mouth upon contact with the saliva without the need for water or munching. Examples of such dosage forms include orodispersible tablets (ODT), and orodispersible films (ODF). The ability to obtain ODF with different dimensions (sizes and thicknesses) makes them a suitable for personalized dosing of single or a fixed-dose combination of drugs in special patient populations. Several biopolymers are currently being exploited in the development of orodispersible dosage forms including alginates due to their versatility, availability, naturally occurring, and biosafety profile. This chapter provides an appraisal on the various applications of alginates in the preparations and their role on the properties of orodispersible dosage forms and highlights future perspectives of this very versatile biopolymer for these innovative drug delivery systems.

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“…Importantly, it was concluded that, when the concentration ratio of HPMC (E5) and PEG400 was 4:3, ODF exhibited the optimal mechanical features, acceptable thickness, disintegration time, and higher Young's modulus values, with lower percent elongation [35]. In another work, a full factorial experimental design was used to incorporate piroxicam into ODFs while studying the results of some formulation factors on the characteristics of the resulting films [36]. These factors were the casting solvent (water or acetone/water mixture), the film-forming agent (HPMC K4M or sodium alginate), and the solubilization system (no solubilizer, L-arginine, poloxamer, or L-arginine/poloxamer mixture).…”

Section: Hydroxypropyl Cellulose (Hpc)mentioning

confidence: 99%

“…Combined use of L-arginine and poloxamer exhibited superior drug dissolution than using each separately. HPMC was more beneficial compared to sodium alginate in terms of mechanical properties and moisture absorption [36]. HPMC (Pharmacoat 606) and various kinds of HPC (Klucel JXF 140 kDa, Klucel EXF 80 kDa, Klucel LXF 95 kDa) were utilized as film-forming polymers in preparation of ibuprofen and loperamide ODFs.…”

Section: Hydroxypropyl Cellulose (Hpc)mentioning

confidence: 99%

“Success Depends on Your Backbone”—About the Use of Polymers as Essential Materials Forming Orodispersible Films

2021

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Polymers constitute a group of materials having a wide-ranging impact on modern pharmaceutical technology. Polymeric components provide the foundation for the advancement of novel drug delivery platforms, inter alia orodispersible films. Orodispersible films are thin, polymeric scraps intended to dissolve quickly when put on the tongue, allowing them to be easily swallowed without the necessity of drinking water, thus eliminating the risk of choking, which is of great importance in the case of pediatric and geriatric patients. Polymers are essential excipients in designing orodispersible films, as they constitute the backbone of these drug dosage form. The type of polymer is of significant importance in obtaining the formulation of the desired quality. The polymers employed to produce orodispersible films must meet particular requirements due to their oral administration and have to provide adequate surface texture, film thickness, mechanical attributes, tensile and folding strength as well as relevant disintegration time and drug release to obtain the final product characterized by optimal pharmaceutical features. A variety of natural and synthetic polymers currently utilized in manufacturing of orodispersible films might be used alone or in a blend. The goal of the present manuscript was to present a review about polymers utilized in designing oral-dissolving films.

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Effect of casting solvent, film-forming agent and solubilizer on orodispersible films of a polymorphic poorly soluble drug: anin vitro/in silicostudy

Cited by 17 publications

References 81 publications

Formulation, characterization, optimization, and in-vivo performance of febuxostat self-nano-emulsifying system loaded sublingual films

Formulation, characterization, optimization, and in-vivo performance of febuxostat self-nano-emulsifying system loaded sublingual films

Applications of Alginates in the Design and Preparation of Orodispersible Dosage Forms

“Success Depends on Your Backbone”—About the Use of Polymers as Essential Materials Forming Orodispersible Films

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