In-Depth Study into Polymeric Materials in Low-Density Gastroretentive Formulations

Iglesias, N.; Galbis, Elsa; Romero-Azogil, Lucía; Benito, Elena; Lucas, Ricardo Dantas de; Garcı́a-Martı́n, Marı́a de Gracia; de-Paz, M.-Violante

doi:10.3390/pharmaceutics12070636

Cited by 39 publications

(33 citation statements)

References 149 publications

(305 reference statements)

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“…For example, Föger and coworkers carried out some in vivo investigations to evaluate a novel oral formulation of PTX based on thiolated polycarbophil [156]. Polycarbophil is the USP/NF compendial name of a family of polyacrylic acids loosely crosslinked with divinyl glycol with broad applications in biomedical and pharmaceutical fields [157], including as a laxative to treat constipation. When thiolated, it was demonstrated that P-gp inhibition was enhanced significantly, thus reducing tumor growth in mammarycancer-induced rats more efficiently than intravenous paclitaxel [156].…”

Section: Thiomer-based Conjugates For Taxanes and Other Anticancer Api Administrationmentioning

confidence: 99%

Thiolated-Polymer-Based Nanoparticles as an Avant-Garde Approach for Anticancer Therapies—Reviewing Thiomers from Chitosan and Hyaluronic Acid

Grosso

de-Paz

2021

Pharmaceutics

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Thiomers (or thiolated polymers) have broken through as avant-garde approaches in anticancer therapy. Their distinguished reactivity and properties, closely linked to their final applications, justify the extensive research conducted on their preparation and use as smart drug-delivery systems (DDSs). Multiple studies have demonstrated that thiomer-rich nanoformulations can overcome major drawbacks found when administering diverse active pharmaceutical ingredients (APIs), especially in cancer therapy. This work focuses on providing a complete and concise review of the synthetic tools available to thiolate cationic and anionic polymers, in particular chitosan (CTS) and hyaluronic acid (HA), respectively, drawing attention to the most successful procedures. Their chemical reactivity and most relevant properties regarding their use in anticancer formulations are also discussed. In addition, a variety of NP formation procedures are outlined, as well as their use in cancer therapy, particularly for taxanes and siRNA. It is expected that the current work could clarify the main synthetic strategies available, with their scope and drawbacks, as well as provide some insight into thiomer chemistry. Therefore, this review can inspire new research strategies in the development of efficient formulations for the treatment of cancer.

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Section: Thiomer-based Conjugates For Taxanes and Other Anticancer Api Administrationmentioning

confidence: 99%

Thiolated-Polymer-Based Nanoparticles as an Avant-Garde Approach for Anticancer Therapies—Reviewing Thiomers from Chitosan and Hyaluronic Acid

Grosso

de-Paz

2021

Pharmaceutics

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“…The melt container had a size of 600 mL, but the capacity can be easily multiplied as needed. The vessel can be heated to 70°C, which makes it suitable for various moldable polymers and materials [26]. The main unit of foaming is the foam cell, where gas is dispersed in the molten dispersion with a high agitation speed.…”

Section: Discussionmentioning

confidence: 99%

Process Optimization for the Continuous Production of a Gastroretentive Dosage Form Based on Melt Foaming

et al. 2021

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Several drugs have poor oral bioavailability due to low or incomplete absorption which is affected by various effects as pH, motility of GI, and enzyme activity. The gastroretentive drug delivery systems are able to deal with these problems by prolonging the gastric residence time, while increasing the therapeutic efficacy of drugs. Previously, we developed a novel technology to foam hot and molten dispersions on atmospheric pressure by a batch-type in-house apparatus. Our aim was to upgrade this technology by a new continuous lab-scale apparatus and confirm that our formulations are gastroretentive. At first, we designed and built the apparatus and continuous production was optimized using a Box–Behnken experimental design. Then, we formulated barium sulfate-loaded samples with the optimal production parameters, which was suitable for in vivo imaging analysis. In vitro study proved the low density, namely 507 mg/cm3, and the microCT record showed high porosity with 40 μm average size of bubbles in the molten suspension. The BaSO4-loaded samples showed hard structure at room temperature and during the wetting test, the complete wetting was detected after 120 min. During the in vivo study, the X-ray taken showed the retention of the formulation in the rat stomach after 2 h. We can conclude that with our device low-density floating formulations were prepared with prolonged gastric residence time. This study provides a promising platform for marketed active ingredients with low bioavailability.

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“…We analyzed the change in the swelling (Equation (3), Figure S3a) and matrix erosion Controlled-release gel-forming matrix tablets are known to undergo swelling and erosion during dissolution. A hydrophilic drug such as Met HCl penetrates and/or diffuses through the hydrated layer of HPMC K15M and is thus released in a controlled manner [68,69]. Erosion also plays an important role in releasing a drug, especially hydrophobic drugs, during dissolution [70].…”

Section: Floating Swelling and Erosion Testing Of The Sustained-release Non-effervescent Floating Tabletmentioning

confidence: 99%

DoE-Based Design of a Simple but Efficient Preparation Method for a Non-Effervescent Gastro-Retentive Floating Tablet Containing Metformin HCl

2021

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A sustained-release non-effervescent floating matrix tablet was prepared using a simple and efficient direct compression of spray-dried granules containing metformin hydrochloride and cetyl alcohol with hydroxypropyl methylcellulose K15M (HPMC K15M). The design of experiments was employed to explore the optimal composition of the tablet. The similarity factor was employed to evaluate the equivalence in dissolution profiles between the test tablets and Glucophage XR as a reference. Bootstrap analysis was used to eliminate the formulations for which the dissolution profile was potentially inequivalent to that of the reference. The optimized tablet consisting of 150 mg of cetyl alcohol and 17% HPMC K15M showed a dissolution profile comparable with that of the reference with a similarity factor of 52.41, exhibited a floating lag time of less than 3 s in buffer media, remained floating for 24 h, and reduced the tablet weight by about 20% compared to that of the reference. The current study sheds light on the potential use of non-effervescent gastro-retentive extended-release tablets for high-dose drugs using a simple and efficient direct compression method, and as a potential alternative treatment for Glucophage XR. This study also highlights the importance of a systematic approach to formulation optimization and the evaluation of the dissolution profile.

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In-Depth Study into Polymeric Materials in Low-Density Gastroretentive Formulations

Cited by 39 publications

References 149 publications

Thiolated-Polymer-Based Nanoparticles as an Avant-Garde Approach for Anticancer Therapies—Reviewing Thiomers from Chitosan and Hyaluronic Acid

Thiolated-Polymer-Based Nanoparticles as an Avant-Garde Approach for Anticancer Therapies—Reviewing Thiomers from Chitosan and Hyaluronic Acid

Process Optimization for the Continuous Production of a Gastroretentive Dosage Form Based on Melt Foaming

DoE-Based Design of a Simple but Efficient Preparation Method for a Non-Effervescent Gastro-Retentive Floating Tablet Containing Metformin HCl

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