Tannic acid as a co-former in co-amorphous systems: Enhancing their physical stability, solubility and dissolution behavior

Fael, Hanan; Demirel, A. Levent

doi:10.1016/j.ijpharm.2020.119284

Cited by 28 publications

(14 citation statements)

References 37 publications

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“…In drug-excipient combinations, the excipients with a small molecular weight, generally called co-formers in this field, act as stabilizers in co-amorphization to enhance the physical stability and dissolution rate of drugs [ 33 , 34 , 35 , 36 , 37 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 ]. The selection of an adequate conformer which can form sufficient intermolecular interactions with the drug, such as charge-assisted interactions and hydrogen bonding, is therefore an important step.…”

Section: Emerging Pharmaceutical Techniques For Amorphization Of Poorly Water-soluble Drugsmentioning

confidence: 99%

“…Along with amino acids, organic acids as co-formers have been explored, such as tannic acid, benzoic acid, malic acid, and citric acid [ 41 , 44 , 45 ]. Wu et al studied the potential of three organic acids, including benzoic acid, malic acid, and citric acid, as co-formers combined with carvedilol, and further found the optimal molar ratio between the organic acids and the drugs in the production of co-amorphous systems [ 44 ].…”

Section: Emerging Pharmaceutical Techniques For Amorphization Of Poorly Water-soluble Drugsmentioning

confidence: 99%

“…Wu et al studied the potential of three organic acids, including benzoic acid, malic acid, and citric acid, as co-formers combined with carvedilol, and further found the optimal molar ratio between the organic acids and the drugs in the production of co-amorphous systems [ 44 ]. Another study found that tannic acid could be used as a co-former to fabricate co-amorphous systems with carbamazepine and indomethacin by successfully forming intermolecular interactions [ 45 ]. From these studies, the potential of organic acids as co-formers was demonstrated.…”

Section: Emerging Pharmaceutical Techniques For Amorphization Of Poorly Water-soluble Drugsmentioning

confidence: 99%

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Recent Technologies for Amorphization of Poorly Water-Soluble Drugs

Kim

Tin

et al. 2021

Pharmaceutics

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Amorphization technology has been the subject of continuous attention in the pharmaceutical industry, as a means to enhance the solubility of poorly water-soluble drugs. Being in a high energy state, amorphous formulations generally display significantly increased apparent solubility as compared to their crystalline counterparts, which may allow them to generate a supersaturated state in the gastrointestinal tract and in turn, improve the bioavailability. Conventionally, hydrophilic polymers have been used as carriers, in which the amorphous drugs were dispersed and stabilized to form polymeric amorphous solid dispersions. However, the technique had its limitations, some of which include the need for a large number of carriers, the tendency to recrystallize during storage, and the possibility of thermal decomposition of the drug during preparation. Therefore, emerging amorphization technologies have focused on the investigation of novel amorphous-stabilizing carriers and preparation methods that can improve the drug loading and the degree of amorphization. This review highlights the recent pharmaceutical approaches utilizing drug amorphization, such as co-amorphous systems, mesoporous particle-based techniques, and in situ amorphization. Recent updates on these technologies in the last five years are discussed with a focus on their characteristics and commercial potential.

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Section: Emerging Pharmaceutical Techniques For Amorphization Of Poorly Water-soluble Drugsmentioning

confidence: 99%

Section: Emerging Pharmaceutical Techniques For Amorphization Of Poorly Water-soluble Drugsmentioning

confidence: 99%

Section: Emerging Pharmaceutical Techniques For Amorphization Of Poorly Water-soluble Drugsmentioning

confidence: 99%

See 1 more Smart Citation

Recent Technologies for Amorphization of Poorly Water-Soluble Drugs

Kim

Tin

et al. 2021

Pharmaceutics

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“…Obviously, the NSP formulation offered a moderate improvement in vitro release when compared with raw CUR, indicating that the solubility of CUR was improved after being prepared into the NSP. The reason for the higher release of TA-CUR-NSP compared with CUR-NSP is that TA improves the solubility of poorly soluble drugs and has an excellent stabilizing effect [37].…”

Section: In Vitro Release Studymentioning

confidence: 99%

Development and Evaluation of Tannic Acid-Coated Nanosuspension for Enhancing Oral Bioavailability of Curcumin

Lee

Bang

et al. 2021

Pharmaceutics

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Curcumin (CUR) has been used in the treatment of various diseases such as cough, fever, skin disease, and infection because of various biological benefits such as anti-inflammatory, antiviral, antibacterial, and antitumor activity. However, CUR is a BCS class 4 group and has a limitation of low bioavailability due to low solubility and permeability. Therefore, the purpose of this study is to prepare a nanosuspension (NSP) loaded with CUR (CUR-NSP) using a statistical design approach to improve the oral bioavailability of CUR, and then to develop CUR-NSP coated with tannic acid to increase the mucoadhesion in the GI tract. Firstly, the optimized CUR-NSP, composed of sodium dodecyl sulfate (SDS) and polyvinylpyrrolidone/vinyl acetate (PVP/VA), was modified with tannic acid (TA). The particle size and polydispersity index of the formulation measured by laser scattering analyzer were 127.7 ± 1.3 nm and 0.227 ± 0.010, respectively. In addition, the precipitation in distilled water (DW) was 1.52 ± 0.58%. Using a differential scanning calorimeter and X-ray diffraction analysis, the stable amorphous form of CUR was confirmed in the formulation, and it was confirmed that CUR-NSP formulation was coated with TA through a Fourier transform-infrared spectroscopy. In the mucoadhesion assay using the turbidity, it was confirmed that TA-CUR-NSP had higher affinity for mucus than CUR-NSP under all pH conditions. This means that the absorption of CUR can be improved by increasing the retention time in the GI tract of the formulation. In addition, the drug release profile showed more than 80% release, and in the cellular uptake study, the absorption of the formulation (TA-CUR-NSP) containing TA acting as an inhibitor of P-gp was increased by 1.6-fold. In the evaluation of antioxidant activity, the SOD activity of TA-CUR-NSP was remarkably high due to TA, which improves cellular uptake and has antioxidant activity. In the pharmacokinetic evaluation, the maximum drug plasma concentration of the TA-coated NSP formulation was 7.2-fold higher than that of the pure drug. In all experiments, it was confirmed that the TA-CUR-NSP is a promising approach to overcome the low oral bioavailability of CUR.

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“…Selain itu, Arginin juga membentuk Gambar 2. Difraktogram PXRD ko-amorf Carbamazepine-Asam Tanat dengan metode physical mixing dan solvent evaporation [49] stabilisasi interaksi π-π dengan molekul yang memiliki cincin aromatik, seperti pada campuran amorf Naproxen-Arginin [41]. Koformer Lisin telah digunakan untuk pembentukan ko-amorf Indometachin melalui metode pembuatan vibration ball.…”

Section: Asam Amino (Aa)unclassified

Pemilihan Jenis Koformer dan Metode Preparasi dalam Sistem Penghantaran Sediaan Ko-Amorf

2021

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Ko-amorf adalah suatu sistem multikomponen padat yang mengandung zat aktif dan molekul dengan berat molekul rendah lainnya (koformer) yang dapat berupa eksipien atau zat aktif yang relevan secara farmakologis. Formulasi ko-amorf yang dibuat dengan metode preparasi dan jenis koformer yang berbeda dapat menghasilkan perbedaan yang signifikan dalam stabilitas fisik dan profil disolusi suatu bentuk ko-amorf. Tujuan penulisan dari artikel review ini adalah untuk menggali informasi lebih dalam tentang sistem ko-amorf, klasifikasi ko-amorf, karakterisasi ko-amorf serta pengaruh jenis koformer dan metode preparasi ko-amorf terhadap pembentukan ko-amorf. Artikel review ini disusun dengan literature search melalui PubMed, MDPI dan Science Direct dengan memasukkan kata kunci co-amorphous, co-amorphous formulations, co-amorphous stabilizers, co-amorphous drug formulations. Dari review ini ditemukan terdapat beberapa jenis koformer yang dapat digunakan untuk pembentukan ko-amorf yaitu dapat berupa zat aktif yang relevan secara farmakologis dan eksipien seperti diantaranya yaitu asam amino, asam karboksilat, asam tanat, quercetin, sakarin dan nikotinamid. Dan untuk metode preparasi ko-amorf yang dapat digunakan diantaranya yaitu ball milling, cryomilling, melt quenching/ quench cooling, hot melt extrusion, solvent evaporation, spray drying, freeze drying hingga teknologi seperti supercritical antisolvent dan microwave technique. Keberhasilan pembentukan ko-amorf ditentukan diantaranya oleh pemilihan jenis koformer yang melibatkan berbagai sifat yang perlu dipertimbangkan, seperti Tg, potensial ikatan hidrogen, ketercampuran/ miscibility, atau perilaku kristalisasi. Sifat zat aktif dan eksipien seperti stabilitas termal, suhu leleh dan kecenderungan kristalisasi zat aktif dan eksipien, menjadi faktor yang perlu diperhatikan dalam pemilihan metode preparasi ko-amorf.

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Tannic acid as a co-former in co-amorphous systems: Enhancing their physical stability, solubility and dissolution behavior

Cited by 28 publications

References 37 publications

Recent Technologies for Amorphization of Poorly Water-Soluble Drugs

Recent Technologies for Amorphization of Poorly Water-Soluble Drugs

Development and Evaluation of Tannic Acid-Coated Nanosuspension for Enhancing Oral Bioavailability of Curcumin

Pemilihan Jenis Koformer dan Metode Preparasi dalam Sistem Penghantaran Sediaan Ko-Amorf

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