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Article ; Online: Formulation and optimization of a single-layer coat for targeting budesonide pellets to the descending Colon.

Soltani, Fatemeh / Kamali, Hossein / Akhgari, Abbas / Afrasiabi Garekani, Hadi / Nokhodchi, Ali / Sadeghi, Fatemeh

Pharmaceutical development and technology

2024 Volume 29, Issue 3, Page(s) 212–220

Abstract: The current budesonide formulations are inadequate for addressing left-sided colitis, and patients might hesitate to use an enema for a prolonged time. This study focuses on developing a single-layer coating for budesonide pellets targeting the ... ...

Abstract	The current budesonide formulations are inadequate for addressing left-sided colitis, and patients might hesitate to use an enema for a prolonged time. This study focuses on developing a single-layer coating for budesonide pellets targeting the descending colon. Pellets containing budesonide (1.5%w/w), PVP K30 (5%w/w), lactose monohydrate (25%w/w) and Avicel pH 102 (68.5%w/w) were prepared using extrusion spheronization technique. Coating formulations were designed using response surface methodology with pH and time-dependent Eudragits. Dissolution tests were conducted at different pH levels (1.2, 6.5, 6.8, and 7.2). Optimal coating formulation, considering coating level and the Eudragit (S + L) ratio to the total coating weight, was determined. Budesonide pellets were coated with the optimized composition and subjected to continuous dissolution testing simulating the gastrointestinal tract. The coating, with 48% S, 12% L, and 40% RS at a 10% coating level, demonstrated superior budesonide delivery to the descending colon. Coated pellets had a spherical shape with a uniform 30 µm thickness coating, exhibiting pH and time-dependent release. Notably, zero-order release kinetics was observed for the last 9 h in colonic conditions. The study suggests that an optimized single-layer coating, incorporating pH and time-dependent polymers, holds promise for consistently delivering budesonide to the descending colon.
MeSH term(s)	Humans ; Budesonide ; Drug Delivery Systems ; Colon ; Colon, Descending ; Solubility ; Drug Implants ; Polymethacrylic Acids
Chemical Substances	Budesonide (51333-22-3) ; methylmethacrylate-methacrylic acid copolymer (25086-15-1) ; Drug Implants ; Polymethacrylic Acids
Language	English
Publishing date	2024-03-06
Publishing country	England
Document type	Journal Article
ZDB-ID	1331774-x
ISSN	1097-9867 ; 1083-7450
ISSN (online)	1097-9867
ISSN	1083-7450
DOI	10.1080/10837450.2024.2321250
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Article: Design and physico-mechanical evaluation of fast-dissolving valsartan polymeric drug delivery system by electrospinning method.

Mohammadreza, Mohammadreza / Iraji, Pariya / Mahmoudi, Zahra / Rahiman, Niloufar / Akhgari, Abbas

Iranian journal of basic medical sciences

2022 Volume 24, Issue 12, Page(s) 1683–1694

Abstract: Objectives: Chronic hypertension is a pervasive morbidity and the leading risk factor for cardiovascular diseases. Valsartan, as an antihypertensive drug, has low solubility and bioavailability. The application of orodispersible films of valsartan is ... ...

Abstract	Objectives: Chronic hypertension is a pervasive morbidity and the leading risk factor for cardiovascular diseases. Valsartan, as an antihypertensive drug, has low solubility and bioavailability. The application of orodispersible films of valsartan is suggested to improve its bioavailability. With this dosage form, the drug dissolves rapidly in saliva and is absorbed readily without the need for water. Materials and methods: For this purpose, valsartan with polyvinylpyrrolidone (PVPK90) polymer were exposed to the electrospinning technique to construct orodispersible nanofilms. The optimum obtained nanofiber, selected by Design-Expert software, was evaluated in terms of mechanical strength for evaluation of the flexibility and fragility of the nanofibers. The drug content, wettability, and disintegration tests, as well as the release assessment of the nanofibers, were performed followed by DSC, FTIR, and XRD assays. Results: The uniform nanofibers' diameter increased with the increase of the polymer concentration. The tensile test verified a stress reduction at the yield point as the polymer concentration increased. Then, the 492 nm nanofiber with above 90% drug encapsulation, containing 8% polymer and 18% valsartan made below 9 kV, was selected. The wetting time was less than 30 sec and over 90% of the drug was released in less than 2 min. The XRD and DSC studies also confirmed higher valsartan solubility due to the construction alternations in nanofibers. The FTIR examination indicated the chemical bonding between the drug and the polymer. Conclusion: The selected nanofibers of valsartan present the essential drug feature and acceptable drug release for further investigations.
Language	English
Publishing date	2022-03-21
Publishing country	Iran
Document type	Journal Article
ZDB-ID	2500485-2
ISSN	2008-3874 ; 2008-3866
ISSN (online)	2008-3874
ISSN	2008-3866
DOI	10.22038/IJBMS.2021.58713.13041
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Article ; Online: A review on curcumin colon-targeted oral drug delivery systems for the treatment of inflammatory bowel disease.

Sardou, Hossein Shahdadi / Vosough, Paria Rahnama / Abbaspour, Mohammadreza / Akhgari, Abbas / Sathyapalan, Thozhukat / Sahebkar, Amirhossein

Inflammopharmacology

2023 Volume 31, Issue 3, Page(s) 1095–1105

Abstract: Synthetic drugs and monoclonal antibodies are the typical treatments to combat inflammatory bowel disease (IBD). However, side effects are present when these treatments are used, and their continued application could be restricted by the high relapse ... ...

Abstract	Synthetic drugs and monoclonal antibodies are the typical treatments to combat inflammatory bowel disease (IBD). However, side effects are present when these treatments are used, and their continued application could be restricted by the high relapse rate of the disease. One potential alternative to these treatments is the use of plant-derived products. The use curcumin is one such treatment option that has seen an increase in usage in treating IBD. Curcumin is derived from a rhizome of turmeric (Curcuma longa), and the results of studies on the use of curcumin to treat IBD are promising. These studies suggest that curcumin interacts with cellular targets such as NF-κB, JAKs/STATs, MAPKs, TNF-α, IL-6, PPAR, and TRPV1 and may reduce the progression of IBD. Potentially, curcumin can be used as a therapeutic agent for patients with IBD when it reduces the incidence of clinical relapse. This review discusses the strategies utilized in designing and developing an oral colonic delivery dosage form of curcumin.
MeSH term(s)	Humans ; Curcumin/pharmacology ; Curcumin/therapeutic use ; Inflammatory Bowel Diseases/drug therapy ; Colon ; Drug Delivery Systems ; NF-kappa B ; Curcuma
Chemical Substances	Curcumin (IT942ZTH98) ; NF-kappa B
Language	English
Publishing date	2023-02-09
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	1080058-x
ISSN	1568-5608 ; 0925-4692
ISSN (online)	1568-5608
ISSN	0925-4692
DOI	10.1007/s10787-023-01140-0
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Article ; Online: Recent progress in the graphene-based biosensing approaches for the detection of Alzheimer's biomarkers.

Rouhi, Nadiyeh / Akhgari, Abbas / Orouji, Neda / Nezami, Alireza / Rahimzadegan, Milad / Kamali, Hossein

Journal of pharmaceutical and biomedical analysis

2022 Volume 222, Page(s) 115084

Abstract: Alzheimer's disease (AD) is one of the most common types of neurodegenerative disorders. It is possible to identify AD early thanks to the measurement of specific biomarker levels. Owing to crucial roles of biomarkers in the AD, the detection of AD- ... ...

Abstract	Alzheimer's disease (AD) is one of the most common types of neurodegenerative disorders. It is possible to identify AD early thanks to the measurement of specific biomarker levels. Owing to crucial roles of biomarkers in the AD, the detection of AD-related biomarkers may be suitable for predictive identification of AD. Biosensors is a novel tool that could be beneficial to appreciate recognition of several AD biomarkers as early as possible. Graphene and its derivatives containing graphene oxide (GO) and reduced-GO (rGO) can be good choice for biosensing approaches due to their unique properties. GO/rGO-based biosensors or nanosensors have been widely used for the determination of AD biomarkers. In this article, the general aspects of AD, its biomarkers, biosensors, and GO are overviewed. In addition, this review provides the current developments in the applications of graphene-based biosensors for recognition of AD biomarkers. Future perspectives and challenges of graphene-based biosensing as a new approach for detection of AD are discussed in brief as well.
MeSH term(s)	Humans ; Graphite ; Alzheimer Disease/diagnosis ; Biosensing Techniques ; Biomarkers
Chemical Substances	graphene oxide ; Graphite (7782-42-5) ; Biomarkers
Language	English
Publishing date	2022-09-28
Publishing country	England
Document type	Journal Article ; Review
ZDB-ID	604917-5
ISSN	1873-264X ; 0731-7085
ISSN (online)	1873-264X
ISSN	0731-7085
DOI	10.1016/j.jpba.2022.115084
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Article: Preparation of stable enteric folic acid-loaded microfiber using the electrospinning method.

Akhgari, Abbas / Iraji, Pariya / Rahiman, Niloufar / Hasanzade Farouji, Akram / Abbaspour, Mohammadreza

Iranian journal of basic medical sciences

2022 Volume 25, Issue 3, Page(s) 405–413

Abstract: Objectives: Folic acid is an essential vitamin, labile to hydrolysis in the acidic environment of the stomach with low water solubility and bioavailability. In order to solve these problems, enteric oral folic acid-loaded microfibers with a pH-sensitive ...

Abstract	Objectives: Folic acid is an essential vitamin, labile to hydrolysis in the acidic environment of the stomach with low water solubility and bioavailability. In order to solve these problems, enteric oral folic acid-loaded microfibers with a pH-sensitive polymer by electrospinning method were prepared. Materials and methods: Electrospinning was performed at different folic acid ratios and voltages. Fibers were evaluated in terms of mechanical strength, acidic resistance, and drug release. Additionally, DSC (Differential Scanning Calorimetry), FTIR (Fourier-transform infrared spectroscopy), and XRD (X-ray diffraction) analyses were performed on the optimal formulation. Results: Drug ratio and voltage had a considerable effect on fibers' entrapment efficiency, acid resistance, and mechanical strength. Based on the obtained results, the optimum formulation containing 1.25% of the drug/polymer was prepared at 18 kV. The entrapment efficiency of the optimal sample was above 90% with an acid resistance of higher than 70%. The tensile test confirmed the high mechanical properties of the optimum microfiber. DSC and XRD tests indicated that folic acid was converted to an amorphous form in the fiber structure and the FTIR test confirmed the formation of a chemical bond between the drug and the polymer. The release of the drug from the optimal fiber was about 90% in 60 min. Conclusion: In conclusion, the optimal formulation of folic acid with proper mechanical properties can be used as a candidate dosage form for further bioavailability investigations.
Language	English
Publishing date	2022-04-05
Publishing country	Iran
Document type	Journal Article
ZDB-ID	2500485-2
ISSN	2008-3874 ; 2008-3866
ISSN (online)	2008-3874
ISSN	2008-3866
DOI	10.22038/IJBMS.2022.61563.13625
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Article ; Online: Corrigendum to "A review on 5-aminosalicylic acid colon-targeted oral drug delivery systems" [Int. J. Pharm. 558 (2019) 367-379].

Shahdadi Sardo, Hossein / Saremnejad, Farinaz / Bagheri, Sara / Akhgari, Abbas / Afrasiabi Garekani, Hadi / Sadeghi, Fatemeh

International journal of pharmaceutics

2022 Volume 628, Page(s) 122312

Language	English
Publishing date	2022-10-28
Publishing country	Netherlands
Document type	Published Erratum
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2022.122312
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Article ; Online: Comparison of 5-ASA layered or matrix pellets coated with a combination of ethylcellulose and eudragits L and s in the treatment of ulcerative colitis in rats.

Sardou, Hossein Shahdadi / Sadeghi, Fatemeh / Garekani, Hadi Afrasiabi / Akhgari, Abbas / Hossein Jafarian, Amir / Abbaspour, Mohammadreza / Nokhodchi, Ali

International journal of pharmaceutics

2023 Volume 640, Page(s) 122981

Abstract: The aim of this study was to evaluate and optimize the combination of time and pH-dependent polymers as a single coating for the design of the colon-specific drug delivery system of 5-aminosalicylic acid (5-ASA) pellets. 5-ASA matrix pellets with a 70% ... ...

Abstract	The aim of this study was to evaluate and optimize the combination of time and pH-dependent polymers as a single coating for the design of the colon-specific drug delivery system of 5-aminosalicylic acid (5-ASA) pellets. 5-ASA matrix pellets with a 70% drug load were prepared by the extrusion-spheronization method. The optimal coating formula which included Eudragit S (ES) + Eudragit L (EL) + Ethylcellulose (EC) was predicted for the targeted drug delivery to the colonic area by a 3
MeSH term(s)	Rats ; Animals ; Mesalamine/chemistry ; Colitis, Ulcerative/chemically induced ; Colitis, Ulcerative/drug therapy ; Solubility ; Colon/physiology ; Drug Delivery Systems ; Drug Implants
Chemical Substances	Mesalamine (4Q81I59GXC) ; methylmethacrylate-methacrylic acid copolymer (25086-15-1) ; ethyl cellulose (7Z8S9VYZ4B) ; Drug Implants
Language	English
Publishing date	2023-04-28
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2023.122981
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Article: Prediction of Optimum Combination of Eudragit RS/Eudragit RL/Ethyl Cellulose Polymeric Free Films Based on Experimental Design for Using as a Coating System for Sustained Release Theophylline Pellets.

Akhgari, Abbas / Tavakol, Ali

Advanced pharmaceutical bulletin

2016 Volume 6, Issue 2, Page(s) 219–225

Abstract: Purpose: The physicochemical properties of free films made from different mixtures of sustained release polymers were investigated, and an optimum formulation coating on drug containing pellets, based on the study of free film was evaluated.: Methods!# ...

Abstract	Purpose: The physicochemical properties of free films made from different mixtures of sustained release polymers were investigated, and an optimum formulation coating on drug containing pellets, based on the study of free film was evaluated. Methods: In order to determine the effect of different variables on the permeability and swelling of films and procedure optimization, the experimental design was fulfilled based on the statistical method of a 3(3) full factorial design, and according to this method 27 formulations were prepared. The films were prepared using casting-solvent evaporation method. Water vapor permeability, the swelling and permeability of free films in both acidic and buffer media, were carried out. Then, the pellets containing theophylline were coated with the optimum formulation. Results: The results of this study demonstrated that an increase in the free film thickness and Eurdragit RS ratio in films lowered the water vapor transmission (WVT), the swelling and the permeability of all formulations, while an increase in the quantity of ethylcellulose, up to a specific ratio (approximately 40%), decreased the permeability and swelling. The most optimum free film formulation was made up of 60% Eudragit RS and 40% ethylcellulose. Conclusion: Pellets coated with a 10% coating level of ethylcellulose and Eudragit RS (4:6) showed suitable release properties and could serve as a favorable sustained release system for theophylline.
Language	English
Publishing date	2016-06-30
Publishing country	Iran
Document type	Journal Article
ZDB-ID	3018440-X
ISSN	2251-7308 ; 2228-5881
ISSN (online)	2251-7308
ISSN	2228-5881
DOI	10.15171/apb.2016.030
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Article: Preparation and Characterization of a Novel Multiparticulate Dosage Form Carrying Budesonide-Loaded Chitosan Nanoparticles to Enhance the Efficiency of Pellets in the Colon.

Soltani, Fatemeh / Kamali, Hossein / Akhgari, Abbas / Ghasemzadeh Rahbardar, Mahboobeh / Afrasiabi Garekani, Hadi / Nokhodchi, Ali / Sadeghi, Fatemeh

Pharmaceutics

2022 Volume 15, Issue 1

Abstract: An attempt was made to conquer the limitation of orally administered nanoparticles for the delivery of budesonide to the colon. The ionic gelation technique was used to load budesonide on chitosan nanoparticles. The nanoparticles were investigated in ... ...

Abstract	An attempt was made to conquer the limitation of orally administered nanoparticles for the delivery of budesonide to the colon. The ionic gelation technique was used to load budesonide on chitosan nanoparticles. The nanoparticles were investigated in terms of size, zeta potential, encapsulation efficiency, shape and drug release. Then, nanoparticles were pelletized using the extrusion-spheronization method and were investigated for their size, mechanical properties, and drug release. Pellets were subsequently coated with a polymeric solution composed of two enteric (eudragit L and S) and time-dependent polymers (eudragit RS) for colon-specific delivery. All formulations were examined for their anti-inflammatory effect in rats with induced colitis and the relapse of the colitis after discontinuation of treatment was also followed. The size of nanoparticles ranged between 288 ± 7.5 and 566 ± 7.7 nm and zeta potential verified their positive charged surface. The drug release from nanoparticles showed an initial burst release followed by a continuous release. Pelletized nanoparticles showed proper mechanical properties and faster drug release in acidic pH compared with alkaline pH. It was interesting to note that pelletized budesonide nanoparticles released the drug throughout the GIT in a sustained fashion, and had long-lasting anti-inflammatory effects while rapid relapse was observed for those treated with conventional budesonide pellets. It seems that there is a synergistic effect of nanoformulation of budesonide and the encapsulation of pelletized nanoparticles in a proper coating system for colon delivery that could result in a significant and long-lasting anti-inflammatory effect.
Language	English
Publishing date	2022-12-26
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2527217-2
ISSN	1999-4923
ISSN	1999-4923
DOI	10.3390/pharmaceutics15010069
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Article ; Online: Screening of different polysaccharides in a composite film based on Eudragit RS for subsequent use as a coating for delivery of 5-ASA to colon.

Shahdadi Sardou, Hossein / Akhgari, Abbas / Afrasiabi Garekani, Hadi / Sadeghi, Fatemeh

International journal of pharmaceutics

2019 Volume 568, Page(s) 118527

Abstract: This study aims at identifying the more suitable polysaccharide in a composite film based on Eudragit RS for 5-ASA delivery to the colon. Different polysaccharides (pectin, chitosan, guar, inulin, and dextran) were examined. The mechanical properties, ... ...

Abstract	This study aims at identifying the more suitable polysaccharide in a composite film based on Eudragit RS for 5-ASA delivery to the colon. Different polysaccharides (pectin, chitosan, guar, inulin, and dextran) were examined. The mechanical properties, swelling index, loss of film mass and permeability of films to 5-ASA were recorded at simulating gastric (SGF), intestinal (SIF) and colonic fluids (SCF). Films containing inulin or dextran were more flexible and showed better mechanical properties. Films containing chitosan, pectin or guar exhibited extensive swelling in SGF and SIF. Loss of film mass and drug permeation was more pronounced in SCF than SIF for all samples indicating their sensitivity to colonic bacteria. However, films containing inulin or dextran showed minimum swelling index in SGF and SIF and the highest ratio of permeability in SCF to SIF. Accordingly, inulin and dextran are suggested as appropriate polysaccharides in a film based on Eudragit RS for colon delivery of 5-ASA.
MeSH term(s)	Acrylic Resins/chemistry ; Animals ; Anti-Inflammatory Agents, Non-Steroidal/chemistry ; Colon/metabolism ; Drug Delivery Systems ; Gastric Juice/chemistry ; Intestinal Secretions/chemistry ; Male ; Mesalamine/chemistry ; Polysaccharides/chemistry ; Rats, Wistar ; Tensile Strength
Chemical Substances	Acrylic Resins ; Anti-Inflammatory Agents, Non-Steroidal ; Polysaccharides ; Eudragit RS (33434-24-1) ; Mesalamine (4Q81I59GXC)
Language	English
Publishing date	2019-07-15
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2019.118527
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