Enteric coating of oral solid dosage forms as a tool to improve drug bioavailability

Maderuelo, Cristina; Lanao, José M.; Zarzuelo, Aránzazu

doi:10.1016/j.ejps.2019.105019

Cited by 92 publications

(96 citation statements)

References 127 publications

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“…In addition, oral solid pharmaceutical forms (tablets, capsules) generally have good physicochemical stability and easy dosing. However, these formulations also face certain obstacles that may impair the bioavailability of the drug such as hepatic first pass effect, complex formation, hydrolysis by gastric pH, gastric and intestinal motility, and drug adsorption and malabsorption due to diseases or surgeries [3][4][5][6]. In addition to these drawbacks, non-adherence to the therapeutic guidelines by the patients is relatively common and makes it harder to achieve drug plasma levels within the therapeutic range [7].…”

Section: Introductionmentioning

confidence: 99%

“…Another factor to consider for oral administration of solid dosage forms is patient acceptance, which can be lower in children and elderly people [8], leading to formulation of oral liquid forms as an alternative. The optimization of these oral pharmaceutical dosage forms has been mostly directed to the prolongation of drug release to reduce the frequency of administration [4]. However, these forms are more complex, from a technological point of view, and any deterioration of them by the patient (i.e., chewing or crushing) or during storage can cause lack of efficacy or even toxicity.…”

Section: Introductionmentioning

confidence: 99%

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Microneedle-Based Delivery: An Overview of Current Applications and Trends

et al. 2020

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Microneedle arrays (MNA) are considered as one of the most promising resources to achieve systemic effects by transdermal delivery of drugs. They are designed as a minimally invasive, painless system which can bypass the stratum corneum, overcoming the potential drawbacks of subcutaneous injections and other transdermal delivery systems such as chemical enhancers, nano and microparticles, or physical treatments. As a trendy field in pharmaceutical and biomedical research, its applications are constantly evolving, even though they are based on very well-established techniques. The number of molecules administered by MNA are also increasing, with insulin and vaccines administration being the most investigated. Furthermore, MNA are being used to deliver cells and applied in other organs and tissues like the eyes and buccal mucosae. This review intends to offer a general overview of the current state of MNA research, focusing on the strategies, applications, and types of molecules delivered recently by these systems. In addition, some information about the materials and manufacturing processes is presented and safety data is discussed.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Microneedle-Based Delivery: An Overview of Current Applications and Trends

et al. 2020

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“…The concept of bioactivity includes the processes of drug entering into systemic circulation, its transportation to the target site, and interactions with different biomolecules, resulting in expression of various metabolic and physiological effects (Wood, 2005 ; Carbonell-Capella et al, 2014 ). Bioavailability is the key aspect for assessment of drug absorption applied via different administration routes (Maderuelo et al, 2019 ).…”

Section: Bioavailability Of Eosmentioning

confidence: 99%

“…Encapsulation of EO is a prerequisite for applying EOs because of some of their properties, such as volatility, intense odor and taste, dose-dependent toxicity, and very high biological activity. The encapsulation also prevents the EOs from degradation and transformation under digestion and protects the body from undesirable effects of EOs (Maderuelo et al, 2019 ). Moreover, entrapping of EOs enhances their bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Natural Macromolecules as Carriers for Essential Oils: From Extraction to Biomedical Application

Stevanović

Sieniawska

Głowniak

et al. 2020

Front. Bioeng. Biotechnol.

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Essential oils (EOs) and their main constituents, the terpenes, are widely studied, mostly relating to their antioxidant ability and bioactivity, such as antimicrobial, anticancer, anti-inflammatory, and range of other actions in the living systems. However, there is limited information on their bioavailability, especially upon clinical studies. Having in mind both strong biological effects and health benefits of EOs and their specific physicochemical properties (volatility, lipophilic character, low water solubility or insolubility, viscosity, expressed odor, concentration-dependent toxicity, etc.), there is a need for their encapsulation for target delivery. Encapsulation of EOs and their constituents is the prerequisite for enhancing their oxidative stability, thermostability, photostability, shelf life, and biological activity. We considered various carrier types such a (1) monophase and polyphase polysaccharide hydrogel carriers, (2) polysaccharide-protein carriers, and (3) lipid carriers in the context of physicochemical and engineering factors. Physicochemical factors are encapsulation efficiency, chemical stability under gastric conditions, mechanical stability, and thermal stability of carrier matrices. Choice of carrier material also determines the encapsulation technique. Consequently, the engineering factors are related to the advantage and disadvantage of various encapsulation techniques frequently used in the literature. In addition, it was intended to address the interactions between (1) main carrier components, such as polysaccharides, proteins, and lipids themselves (in order to form chemically and mechanically stable structure); (2) main carrier components with pepsin under gastric conditions (in order to form resistant material under gastric conditions); and (3) main carrier components with EOs (in order to enhance encapsulation efficiency), as a necessary precondition for whole process optimization. Finally, different sources for obtaining natural carrier macromolecules are surveyed, especially the agro-waste materials and agricultural and food by-products. This review article highlights the bioavailability aspects of encapsulated EOs and physicochemical and engineering factors concerning natural macromolecule carriers for their target delivery and application.

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“…The enteric-coating systems use different excipients that are insoluble in the gastric media in order to prevent or to delay the release of the active pharmaceutical ingredient (API) in the stomach [12]. Generally, the gastro-resistance is needed either to protect sensitive APIs, such as proton pump inhibitors or erythromycin from degradation in acidic media [2,13,15] or to protect the stomach mucosa from the irritative effect of the drug [4].…”

Section: Introductionmentioning

confidence: 99%

Evaluation of the Impact of the Inlet Air Humidity During Coating Step on the in Vitro Dissolution of Modified-Release Film-Coated Pellets Containing a BCS Class I Active Substance

Dumitrașcu¹

2020

FARMACIA

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Present study aimed to evaluate the impact of the inlet air humidity during the coating step on the in vitro release profile of modified-release film-coated pellets containing a BCS class I active substance, by assessing the results obtained for 25 experimental batches. In order to ensure both the delayed and the prolonged-release mechanism, the release controlling agent (metacrylic acid-ethyl acrylate copolymer in a 1:1 ratio) was added in both matrix pellets and film-coat. The gastro-resistance of the pellets was evaluated after 2 hours in acidic media according to the in-force EMEA and FDA Guidelines. Based on the results obtained for 22 experimental batches, it can be concluded that the optimum absolute humidity of the inlet air during coating should be above 4.5 g/kg, in order to provide an acidic barrier for the pellets. A lower value for the absolute humidity of the inlet air during the coating process increase the brittleness of the coating and therefore reduces its barrier capabil ity. Three experimental batches were manufactured by reducing the inlet air volume and the inlet temperature and by increasing the spray rate, therefore by reducing the product temperature at which the coating is form. The changes in the manufacturing process reduced the impact of a lower inlet air humidity during, but the dependency was not completely cancelled. Rezumat Prezentul studiu a avut ca scop evaluarea impactului umidității aerului de intrare în timpul etapei de filmare asupra profilului de cedare in vitro a unei substanțe active model ușor solubile, aparținând clasei I a Sistemului de Clasificare Biofarmaceutică, din peletele filmate cu eliberare modificată. Evaluarea s-a realizat prin procesarea rezultatelor obținute pentru 25 de loturi experimentale de pelete. Pentru a asigura atât caracterul enterosolubil, cât și cedarea prelungită a peletelor, a fost utilizat un amestec acid metacrilic-copolimer acrilat de etil în raport 1:1, care a fost adăugat atât în matricea peletelor cât și în filmul exterior. Gastro-rezistența a fost evaluată după 2 ore în mediu acid în conformitate cu reglementările în vigoare. Pe baza rezultatelor obținute pentru 22 de loturi experimentale, s-a putut concluziona că umiditatea absolută optimă a aerului de intrare în timpul procesului de filmare ar trebui să fie peste 4,5 g/kg. O valoare mai mică pentru umiditatea absolută a aerului crește friabilitatea filmului și, prin urmare, reduce capacitatea de barieră a acestuia. Trei serii experimentale au fost fabricate prin reducerea debitului aerului de intrare, reducerea temperaturii aerului de întrare și creșterea debitului de acoperire, lucru care a generat reducerea temperaturii în produs la care se formează filmul de acoperire. Schimbările în procesul de fabricație au redus impactul negativ al unei umidități mai mici a aerului, dar influența acestuia nu a fost complet anulată.

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Enteric coating of oral solid dosage forms as a tool to improve drug bioavailability

Cited by 92 publications

References 127 publications

Microneedle-Based Delivery: An Overview of Current Applications and Trends

Microneedle-Based Delivery: An Overview of Current Applications and Trends

Natural Macromolecules as Carriers for Essential Oils: From Extraction to Biomedical Application

Evaluation of the Impact of the Inlet Air Humidity During Coating Step on the in Vitro Dissolution of Modified-Release Film-Coated Pellets Containing a BCS Class I Active Substance

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