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Pharmaceutics
Special Issues
New Formulation for Acute and Chronic Inflammatory Diseases
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New Formulation for Acute and Chronic Inflammatory Diseases

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: closed (30 April 2022) | Viewed by 9720

Special Issue Editors

Prof. Dr. Ana C. Calpena

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Guest Editor
Department of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028 Barcelona, Spain
Interests: topical drug delivery systems; dermal absorption; skin models; in vitro studies; nanomedicine; transdermal delivery; transmucosal delivery; cronocosmetic
Special Issues, Collections and Topics in MDPI journals
Dr. Marcelle Silva-Abreu

E-Mail Website
Guest Editor
1. Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028 Barcelona, Spain
2. Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, 08028 Barcelona, Spain
Interests: nanotechnology; inflammation diseases; drug delivery systems; nanoemulsions; polymeric and lipidic systems; oral and topical dosage forms

Special Issue Information

Dear Colleagues,

Inflammation could be defined by a physical factor that triggers an immune reaction in living tissue. It is the process by which the immune system recognizes and removes harmful stimuli and initiates the healing process. Inflammation can be divided into two types, acute and chronic, the latter being able to contribute to a wide range of diseases such as intestinal diseases, diabetes, asthma, osteoarthritis, cardiovascular diseases, allergies, Alzheimer’s, autoimmune disorders, and lung diseases, among others. Different alternatives of pharmaceutical formulations have been used for the treatment where inflammation has its main role, as well as drug delivery systems, including liposomes, nanoparticles (lipid and polymeric), nanocrystals, dendrimers, niosomes, and micelles. In addition, dosage forms such as semi-solid, solid, liquid, oral and topical formulations have  historically been used with excellent results. This Special Issue serves to highlight and capture the continuous progress and the current situation of different new pharmaceutical formulations for the treatment of inflammatory diseases. We invite articles on all aspects of acute and chronic inflammation using different pharmaceutical formulations, including diverse routes of administration.

Prof. Dr. Ana C. Calpena
Dr. Marcelle Silva-Abreu
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • nanomedicine
  • anti-inflammatory formulation
  • oral and topical
  • ophthalmic
  • parenteral
  • inhalation
  • rectal
  • solid
  • semi-solid
  • liquid

Published Papers (4 papers)

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Research

22 pages, 2476 KiB  
Article
Multi-Strain-Probiotic-Loaded Nanoparticles Reduced Colon Inflammation and Orchestrated the Expressions of Tight Junction, NLRP3 Inflammasome and Caspase-1 Genes in DSS-Induced Colitis Model
by Abdullah Glil Alkushi, Sara T. Elazab, Ahmed Abdelfattah-Hassan, Hala Mahfouz, Gamal A. Salem, Nagwa I. Sheraiba, Eman A. A. Mohamed, Mai S. Attia, Eman S. El-Shetry, Ayman A. Saleh, Naser A. ElSawy and Doaa Ibrahim
Pharmaceutics 2022, 14(6), 1183; https://doi.org/10.3390/pharmaceutics14061183 - 31 May 2022
Cited by 16 | Viewed by 2820
Abstract
Gut modulation by multi-strain probiotics (MSPs) is considered an effective strategy for treating inflammatory bowel disease (IBD). The combination of nanomaterial-based MSPs can improve their viability and resistance and can allow their targeted release in the gastrointestinal tract to be achieved. Thus, our [...] Read more.
Gut modulation by multi-strain probiotics (MSPs) is considered an effective strategy for treating inflammatory bowel disease (IBD). The combination of nanomaterial-based MSPs can improve their viability and resistance and can allow their targeted release in the gastrointestinal tract to be achieved. Thus, our aim is to investigate the prospective role of MSP integration into nanomaterials (MSPNPs) and the underlying molecular mechanisms supporting their application as an alternative therapy for IBD using a colitis rat model. To induce the colitis model, rats received 5% DSS, and the efficacy of disease progression after oral administration of MSPNPs was assessed by evaluating the severity of clinical signs, inflammatory response, expressions of tight-junction-related genes and NLRP3 inflammasome and caspase-1 genes, microbial composition and histopathological examination of colonic tissues. The oral administration of MSPNPs successfully alleviated the colonic damage induced by DSS as proved by the reduced severity of clinical signs and fecal calprotectin levels. Compared with the untreated DSS-induced control group, the high activities of colonic NO and MPO and serum CRP levels were prominently reduced in rats treated with MSPNPs. Of note, colonic inflammation in the group treated with MSPNPs was ameliorated by downstreaming NLRP3 inflammasome, caspase-1, IL-18 and IL-1β expressions. After colitis onset, treatment with MSPNPs was more effective than that with free MSPs in restoring the expressions of tight-junction-related genes (upregulation of occludin, ZO-1, JAM, MUC and FABP-2) and beneficial gut microbiota. Interestingly, treatment with MSPNPs accelerated the healing of intestinal epithelium as detected in histopathological findings. In conclusion, the incorporation of MPSs into nanomaterials is recommended as a perspective strategy to overcome the challenges they face and augment their therapeutic role for treating of colitis. Full article
(This article belongs to the Special Issue New Formulation for Acute and Chronic Inflammatory Diseases)
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16 pages, 1933 KiB  
Article
Swine as the Animal Model for Testing New Formulations of Anti-Inflammatory Drugs: Carprofen Pharmacokinetics and Bioavailability of the Intramuscular Route
by Lidia Gómez-Segura, Antoni Boix-Montañes, Mireia Mallandrich, Alexander Parra-Coca, José L. Soriano-Ruiz, Ana Cristina Calpena, Álvaro Gimeno, David Bellido and Helena Colom
Pharmaceutics 2022, 14(5), 1045; https://doi.org/10.3390/pharmaceutics14051045 - 12 May 2022
Cited by 3 | Viewed by 1963
Abstract
Carprofen (CP) is a non-steroidal anti-inflammatory drug (NSAID) frequently used to treat respiratory diseases in numerous small animals, but also in large species. CP is a formidable candidate for further therapeutic research of human inflammatory diseases using the pig as an animal model. [...] Read more.
Carprofen (CP) is a non-steroidal anti-inflammatory drug (NSAID) frequently used to treat respiratory diseases in numerous small animals, but also in large species. CP is a formidable candidate for further therapeutic research of human inflammatory diseases using the pig as an animal model. However, CP administration in swine is very uncommon and respective pharmacokinetics/bioavailability studies are scarce. A simultaneous population pharmacokinetic analysis after CP intravenous and intramuscular administrations in pigs has shown high extent and rate of absorption and a similar distribution profile with respect to man and other mammals. However, clearance and half-life values found in swine suggest a slower elimination process than that observed in man and some other animal species. Although not reported in other species, liver and kidney concentrations achieved at 48 h post-intramuscular administration in pigs were ten times lower than those found in plasma. Simulations pointed to 4 mg/kg every 24 h as the best dosage regimen to achieve similar therapeutic levels to those observed in other animal species. All these findings support the use of pig as an animal model to study the anti-inflammatory effects of CP in humans. Full article
(This article belongs to the Special Issue New Formulation for Acute and Chronic Inflammatory Diseases)
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17 pages, 2734 KiB  
Article
Effect of Penetration Enhancers and Safety on the Transdermal Delivery of Apremilast in Skin
by Paulo Sarango-Granda, Lupe Carolina Espinoza, Natalia Díaz-Garrido, Helen Alvarado, María J. Rodríguez-Lagunas, Laura Baldomá and Ana Calpena
Pharmaceutics 2022, 14(5), 1011; https://doi.org/10.3390/pharmaceutics14051011 - 07 May 2022
Cited by 8 | Viewed by 2655
Abstract
The poor water solubility of apremilast (APR) is the main impediment to the penetration of the drug through the skin barrier. The objective of this study was to evaluate the permeability of APR in different solutions enriched with penetration promoters in ex vivo [...] Read more.
The poor water solubility of apremilast (APR) is the main impediment to the penetration of the drug through the skin barrier. The objective of this study was to evaluate the permeability of APR in different solutions enriched with penetration promoters in ex vivo samples of human skin, and additionally assess its tolerance in vivo. To this end, APR solutions with 5% promoter were developed, and the drug’s ability to penetrate human abdominal skin samples was evaluated; the coefficients of permeability, cumulated amounts permeated, and flow were some of the parameters evaluated; likewise, the in vitro and in vivo tolerance of the solutions was evaluated. The results obtained showed that the solutions containing squalene as a promoter improved the penetration of APR compared to the other promoters evaluated; in the same way, on an in vitro scale in HaCaT cells, the promoters were not toxic, finding a cell viability greater than 80% at the different dilutions evaluated. In the in vivo tests carried out with the solution that presented the best results (APR-Squalene solution), it was observed that it does not cause irritation or erythema on the skin after its colorimetric and histological evaluation of the dorsal region of rats after its application. Squalene becomes an excellent candidate to improve the permeability of the drug in the case of the development of a topical formulation; in addition, it was confirmed that this penetration enhancer is neither toxic nor irritating when in contact with the skin in in vivo tests. Full article
(This article belongs to the Special Issue New Formulation for Acute and Chronic Inflammatory Diseases)
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18 pages, 7857 KiB  
Article
Stabilization by Nano Spray Dryer of Pioglitazone Polymeric Nanosystems: Development, In Vivo, Ex Vivo and Synchrotron Analysis
by Marcelle Silva-Abreu, Esther Miralles, Christina S. Kamma-Lorger, Marta Espina, María Luisa García and Ana Cristina Calpena
Pharmaceutics 2021, 13(11), 1751; https://doi.org/10.3390/pharmaceutics13111751 - 20 Oct 2021
Cited by 3 | Viewed by 1614
Abstract
Pioglitazone-loaded PLGA-PEG nanoparticles (NPs) were stabilized by the spray drying technique as an alternative to the treatment of ocular inflammatory disorders. Pioglitazone-NPs were developed and characterized physiochemically. Interaction studies, biopharmaceutical behavior, ex vivo corneal and scleral permeation, and in vivo bioavailability evaluations were [...] Read more.
Pioglitazone-loaded PLGA-PEG nanoparticles (NPs) were stabilized by the spray drying technique as an alternative to the treatment of ocular inflammatory disorders. Pioglitazone-NPs were developed and characterized physiochemically. Interaction studies, biopharmaceutical behavior, ex vivo corneal and scleral permeation, and in vivo bioavailability evaluations were conducted. Fibrillar diameter and interfibrillar corneal spacing of collagen was analyzed by synchrotron X-ray scattering techniques and stability studies at 4 °C and was carried out before and after the spray drying process. NPs showed physicochemical characteristics suitable for ocular administration. The release was sustained up to 46 h after drying; ex vivo corneal and scleral permeation profiles of pioglitazone-NPs before and after drying demonstrated higher retention and permeation through cornea than sclera. These results were correlated with an in vivo bioavailability study. Small-angle X-ray scattering (SAXS) analysis did not show a significant difference in the organization of the corneal collagen after the treatment with pioglitazone-NPs before and after the drying process, regarding the negative control. The stabilization process by Nano Spray Dryer B-90 was shown to be useful in preserving the activity of pioglitazone inside the NPs, maintaining their physicochemical characteristics, in vivo bioavailability, and non-damage to corneal collagen function after SAXS analysis was observed. Full article
(This article belongs to the Special Issue New Formulation for Acute and Chronic Inflammatory Diseases)
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