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  1. Article ; Online: Anti-Inflammatory Properties of Drugs Used to Control COVID-19 and their Effects on the Renin-Angiotensin System and Angiotensin-Converting Enzyme-2.

    Gilzad-Kohan, Hamed / Jamali, Fakhreddin

    Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques

    2020  Volume 23, Page(s) 259–277

    Abstract: COVID-19 infection is associated with systemic inflammation, and sometimes hyperinflammatory responses with cytokine storm. This plays a major role in COVID-19 severity and poor disease prognosis, even death. Higher levels of inflammatory hallmarks ... ...

    Abstract COVID-19 infection is associated with systemic inflammation, and sometimes hyperinflammatory responses with cytokine storm. This plays a major role in COVID-19 severity and poor disease prognosis, even death. Higher levels of inflammatory hallmarks including C-reactive protein, ferritin, D-dimers, and cytokines such as interleukin (IL) -6, IL-10 and tumor necrosis factor- α (TNF-α) have been reported. Many anti-viral drugs have been tried, but none were proven fully effective. Supportive care and management of the complications that are caused mainly by inflammation might be the key to greater survival rates and shorter hospitalization (e.g., the use of remdesivir, lopinavir, ritonavir, umifenovir (arbidol), oseltamivir, ganciclovir, favipiravir, darunavir, hydroxychloroquine, chloroquine, colchicine, azithromycin, anakinra, canakinumab, tocilizumab, siltuximab, sarilumab, Type 1 interferon, interferon β-1a, interferon α- 2b, baricitinib, ruxolitinib, fedratinib, methylprednisolone and dexamethasone). However, the efficacy of these treatments still needs well-planned clinical trials. In such trials, careful attention must be paid to the duration of the treatment, the onset of beneficial effects, and the severity of the disease, otherwise, the outcomes may still remain inconclusive. Herein, we present a review of the current drugs, which are being used in the management of the disease and their anti-inflammatory properties. We also investigated if these drugs directly interact with Angiotensin-Converting Enzyme (ACE 2), which is a crucial component of the virus entry to the cells.
    MeSH term(s) Anti-Inflammatory Agents/administration & dosage ; Anti-Inflammatory Agents/pharmacology ; Antiviral Agents/administration & dosage ; Antiviral Agents/pharmacology ; Coronavirus Infections/drug therapy ; Coronavirus Infections/virology ; Humans ; Inflammation/drug therapy ; Inflammation/virology ; Pandemics ; Peptidyl-Dipeptidase A/metabolism ; Pneumonia, Viral/drug therapy ; Pneumonia, Viral/virology ; Renin-Angiotensin System/drug effects
    Chemical Substances Anti-Inflammatory Agents ; Antiviral Agents ; Peptidyl-Dipeptidase A (EC 3.4.15.1) ; angiotensin converting enzyme 2 (EC 3.4.17.-)
    Keywords covid19
    Language English
    Publishing date 2020-07-31
    Publishing country Canada
    Document type Journal Article ; Review
    ISSN 1482-1826
    ISSN (online) 1482-1826
    DOI 10.18433/jpps31346
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Revolutionizing pharmacokinetics: the dawn of AI-powered analysis.

    Ghayoor, Ali / Kohan, Hamed Gilzad

    Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques

    2024  Volume 27, Page(s) 12671

    Abstract: This editorial explores how artificial intelligence (AI) is revolutionizing the science of pharmacokinetics (PK). It discusses the challenges of conventional PK analysis and how AI has transformed this area. It highlights the promise of artificial ... ...

    Abstract This editorial explores how artificial intelligence (AI) is revolutionizing the science of pharmacokinetics (PK). It discusses the challenges of conventional PK analysis and how AI has transformed this area. It highlights the promise of artificial intelligence (AI) in predicting pharmacokinetic profiles from chemical structures and its application in several aspects of pharmacology, including dosage customization and drug interactions. Additionally, it emphasizes how important ethical issues and openness are to AI applications, especially when it comes to pharmacokinetic prediction and dataset adaptation. Future directions for AI in PK are discussed, with the creation of all-inclusive AI pharmacokinetics/pharmacometrics software being envisioned. Drug discovery and patient care could be transformed toward more individualized and effective healthcare solutions with the help of this software, which could handle tasks such as data cleaning, model selection, and regulatory report preparation. The editorial highlights the importance of AI in improving pharmaceutical sciences while urging caution and teamwork in navigating its possible uses in pharmacokinetics.
    MeSH term(s) Humans ; Artificial Intelligence ; Software ; Drug Discovery
    Language English
    Publishing date 2024-02-16
    Publishing country Switzerland
    Document type Editorial
    ZDB-ID 1422972-9
    ISSN 1482-1826 ; 1482-1826
    ISSN (online) 1482-1826
    ISSN 1482-1826
    DOI 10.3389/jpps.2024.12671
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Anti-Inflammatory Properties of Drugs Used to Control COVID-19 and their Effects on the Renin-Angiotensin System and Angiotensin-Converting Enzyme-2

    Hamed Gilzad-Kohan / Fakhreddin Jamali

    Journal of Pharmacy & Pharmaceutical Sciences, Vol 23, Iss

    2020  Volume 1

    Abstract: COVID-19 infection is associated with systemic inflammation, and sometimes hyperinflammatory responses with cytokine storm. This plays a major role in COVID-19 severity and poor disease prognosis, even death. Higher levels of inflammatory hallmarks ... ...

    Abstract COVID-19 infection is associated with systemic inflammation, and sometimes hyperinflammatory responses with cytokine storm. This plays a major role in COVID-19 severity and poor disease prognosis, even death. Higher levels of inflammatory hallmarks including C-reactive protein, ferritin, D-dimers, and cytokines such as interleukin (IL) -6, IL-10 and tumor necrosis factor- α (TNF-α) have been reported. Many anti-viral drugs have been tried, but none were proven fully effective. Supportive care and management of the complications that are caused mainly by inflammation might be the key to greater survival rates and shorter hospitalization (e.g., the use of remdesivir, lopinavir, ritonavir, umifenovir (arbidol), oseltamivir, ganciclovir, favipiravir, darunavir, hydroxychloroquine, chloroquine, colchicine, azithromycin, anakinra, canakinumab, tocilizumab, siltuximab, sarilumab, Type 1 interferon, interferon β-1a, interferon α-2b, baricitinib, ruxolitinib, fedratinib, methylprednisolone and dexamethasone). However, the efficacy of these treatments still needs well-planned clinical trials. In such trials, careful attention must be paid to the duration of the treatment, the onset of beneficial effects, and the severity of the disease, otherwise, the outcomes may still remain inconclusive. Herein, we present a review of the current drugs, which are being used in the management of the disease and their anti-inflammatory properties. We also investigated if these drugs directly interact with Angiotensin-Converting Enzyme (ACE 2), which is a crucial component of the virus entry to the cells.
    Keywords Therapeutics. Pharmacology ; RM1-950 ; Pharmacy and materia medica ; RS1-441 ; covid19
    Subject code 610
    Language English
    Publishing date 2020-07-01T00:00:00Z
    Publisher Canadian Society for Pharmaceutical Sciences
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  4. Article: Anti-Inflammatory Properties of Drugs Used to Control COVID-19 and their Effects on the Renin-Angiotensin System and Angiotensin-Converting Enzyme-2

    Gilzad-Kohan, Hamed / Jamali, Fakhreddin

    J Pharm Pharm Sci

    Abstract: COVID-19 infection is associated with systemic inflammation, and sometimes hyperinflammatory responses with cytokine storm. This plays a major role in COVID-19 severity and poor disease prognosis, even death. Higher levels of inflammatory hallmarks ... ...

    Abstract COVID-19 infection is associated with systemic inflammation, and sometimes hyperinflammatory responses with cytokine storm. This plays a major role in COVID-19 severity and poor disease prognosis, even death. Higher levels of inflammatory hallmarks including C-reactive protein, ferritin, D-dimers, and cytokines such as interleukin (IL) -6, IL-10 and tumor necrosis factor- α (TNF-α) have been reported. Many anti-viral drugs have been tried, but none were proven fully effective. Supportive care and management of the complications that are caused mainly by inflammation might be the key to greater survival rates and shorter hospitalization (e.g., the use of remdesivir, lopinavir, ritonavir, umifenovir (arbidol), oseltamivir, ganciclovir, favipiravir, darunavir, hydroxychloroquine, chloroquine, colchicine, azithromycin, anakinra, canakinumab, tocilizumab, siltuximab, sarilumab, Type 1 interferon, interferon ß-1a, interferon α- 2b, baricitinib, ruxolitinib, fedratinib, methylprednisolone and dexamethasone). However, the efficacy of these treatments still needs well-planned clinical trials. In such trials, careful attention must be paid to the duration of the treatment, the onset of beneficial effects, and the severity of the disease, otherwise, the outcomes may still remain inconclusive. Herein, we present a review of the current drugs, which are being used in the management of the disease and their anti-inflammatory properties. We also investigated if these drugs directly interact with Angiotensin-Converting Enzyme (ACE 2), which is a crucial component of the virus entry to the cells.
    Keywords covid19
    Publisher WHO
    Document type Article
    Note WHO #Covidence: #690524
    Database COVID19

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  5. Article ; Online: Monkeypox: Virology, Pathophysiology, Clinical Characteristics, Epidemiology, Vaccines, Diagnosis, and Treatments.

    Soheili, Marzieh / Nasseri, Sherko / Afraie, Maryam / Khateri, Sorour / Moradi, Yousef / Mahdavi Mortazavi, Seyede Maryam / Gilzad-Kohan, Hamed

    Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques

    2022  Volume 25, Page(s) 297–322

    Abstract: The World Health Organization, has declared the recent multiregional outbreak of monkeypox, a global public health emergency. Monkeypox is a zoonotic viral infection endemic to the west and central Africa. It belongs to the Poxviridae family, the ... ...

    Abstract The World Health Organization, has declared the recent multiregional outbreak of monkeypox, a global public health emergency. Monkeypox is a zoonotic viral infection endemic to the west and central Africa. It belongs to the Poxviridae family, the Chordopoxvirinae subfamily, and the Orthopoxvirus genus. The Poxviridae family generally consists of complex, large, enveloped, and linear double-stranded DNA viruses. The initial clinical symptoms of monkeypox are often fever, severe headache, lymphadenopathy, myalgia, and fatigue. The skin lesions typically erupt within 1-3 days of the onset of fever. The rash tends to be more localized on the face and extremities than on the trunk. Monkeypox is often a self-limiting infection, and symptoms last from 2 to 4 weeks. It is isolated from various species, but the exact natural host is uncertain. Monkeypox is transmitted by close contact with infected humans or animals. Currently, no specific medication is available for monkeypox, and the existing therapeutics are the anti-viral agents approved for smallpox infection, including tecovirimat, cidofovir, and brincidofovir. Additionally, the U.S. Food and Drug Administration has approved Vaccinia Immune Globulin Intravenous for treating vaccination complications. It is diagnosed by PCR. There are currently two vaccines licensed by the U.S. Food and Drug Administration. According to the WHO guidance, the first-generation smallpox vaccines held in national reserves of some countries are not recommended as they do not meet the current safety and manufacturing standards. The interim guidance indicates that new and safer (second- and third generation) vaccines for smallpox, may be beneficial for monkeypox prevention, including JYNNEOS, which has been approved for the prevention of monkeypox. Human monkeypox was first reported in 1970. Since then, it has caused several outbreaks, mainly in central and west Africa. The first monkeypox outbreak outside of Africa occurred in the United States in 2003, linked to contact with infected pet prairie dogs. More recently (2018-2021), monkeypox cases have been reported in travelers from Nigeria to the United Kingdom, Israel, Singapore, and the US. Since May 2022, multiple monkeypox cases have been confirmed in several non-endemic countries, raising the concern of an emerging global pandemic. This review is an updated overview of our current state of knowledge regarding monkeypox virology, pathophysiology, clinical characteristics, epidemiology, vaccines, diagnosis, and treatment options.
    MeSH term(s) Animals ; Cidofovir ; DNA ; Humans ; Mpox (monkeypox)/diagnosis ; Mpox (monkeypox)/drug therapy ; Mpox (monkeypox)/epidemiology ; Smallpox ; United States ; Vaccines
    Chemical Substances Vaccines ; DNA (9007-49-2) ; Cidofovir (JIL713Q00N)
    Language English
    Publishing date 2022-09-21
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 1422972-9
    ISSN 1482-1826 ; 1482-1826
    ISSN (online) 1482-1826
    ISSN 1482-1826
    DOI 10.18433/jpps33138
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Calcitriol Reverses Induced Expression of Efflux Proteins and Potentiates Cytotoxic Activity of Gemcitabine in Capan-2 Pancreatic Cancer Cells.

    Gilzad-Kohan, Hamed / Sani, Shabnam / Boroujerdi, Mehdi

    Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques

    2017  Volume 20, Page(s) 295–304

    Abstract: Purpose: Efflux and influx proteins play a major role in chemo-resistance by affecting the net cellular uptake of anti-cancer drugs. Hence, alteration of the efflux and influx protein expression may result in variations of chemotherapeutics uptake and ... ...

    Abstract Purpose: Efflux and influx proteins play a major role in chemo-resistance by affecting the net cellular uptake of anti-cancer drugs. Hence, alteration of the efflux and influx protein expression may result in variations of chemotherapeutics uptake and consequently cell death rate. The present study investigated the effects of pre-treatment of capan-2 pancreatic cancer cells with calcitriol, butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA) or silibinin on the induction of three major efflux proteins and the main gemcitabine influx protein. The influence of the pre-treatments on the net cellular uptake of gemcitabine, total ATPase activity, and cell death rate were also evaluated.
    Methods: Capan-2 pancreatic cancer cells were pre-treated for 24 h with calcitriol, BHT, BHA, or silibinin, followed by gemcitabine treatment. The concentration of gemcitabine was quantified using ultra-performance liquid chromatography (UPLC). Real-time polymerase chain reaction (RT-PCR) was utilized in order to investigate the expression of the mRNAs. The expression of the proteins was assessed using western blotting. Measurement of the ATPase activity was conducted utilizing a colorimetric method and viability of the cells was determined using a luminescent cell viability assay.
    Results: Protein expression studies showed that BHT, silibinin, and BHA increased expression of the efflux proteins and decreased the overall uptake of gemcitabine, whereas calcitriol significantly inhibited expression of the efflux proteins and increased gemcitabine uptake. Expression of specific mRNAs correlated reasonably well with the levels of corresponding proteins. Additionally, the expression of efflux proteins and ATPase activity were well correlated, signifying that the induced efflux proteins are functionally active. Moreover, pre-treatment with calcitriol resulted in a significant increase in cell death with gemcitabine treatment, whereas, BHA significantly reduced the cell death rate. On the other hand, pre-treatment with BHT and silibinin had no significant effect on the cell death rate.
    Conclusions: Pre-treatment of the pancreatic cancer cells with calcitriol significantly increased gemcitabine cellular uptake and consequently decreased cell viability after treatment with gemcitabine, whereas BHA significantly reduced gemcitabine uptake and decreased cell death rate, which were at least partially attributed to the alteration of expression of efflux and influx proteins. This article is open to POST-PUBLICATION REVIEW. Registered readers (see "For Readers") may comment by clicking on ABSTRACT on the issue's contents page.
    Language English
    Publishing date 2017
    Publishing country Canada
    Document type Journal Article
    ISSN 1482-1826
    ISSN (online) 1482-1826
    DOI 10.18433/J37W7R
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article ; Online: The Effect of HIV/AIDS Infection on the Clinical Outcomes of COVID-19: A Meta-Analysis.

    Moradi, Yousef / Soheili, Marzieh / Dehghanbanadaki, Hojat / Moradi, Ghobad / Moradpour, Farhad / Mahdavi Mortazavi, Seyede Maryam / Gilzad Kohan, Hamed / Zareie, Mostafa

    Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques

    2022  Volume 25, Page(s) 183–192

    Abstract: Purpose: Patients with HIV may be more likely to become severely ill from COVID-19. The present meta-analysis aims to determine the impact of HIV/AIDS infection on the clinical outcomes of COVID-19.: Methods: A comprehensive literature search was ... ...

    Abstract Purpose: Patients with HIV may be more likely to become severely ill from COVID-19. The present meta-analysis aims to determine the impact of HIV/AIDS infection on the clinical outcomes of COVID-19.
    Methods: A comprehensive literature search was performed to identify relevant cohort studies to evaluate the association of HIV/AIDS infection with clinical outcomes of COVID-19. International databases, including PubMed (Medline), Web of Sciences, Scopus, and Embase, were searched from the emergence of the COVID-19 pandemic until January 2022. We utilized the risk ratio (RR) with its 95% confidence interval (95% CI) to quantify the effect of cohort studies.
    Results: Twelve cohort studies were included in this meta-analysis, which examined a total number of 17,786,384 patients. Among them, 40,386 were identified to be HIV positive, and 17,745,998 were HIV negative. The pooled analyses showed HIV positive patients who were co-infected with SARS-CoV-2 were 58% more likely to develop a fever (RR=1.58; 95% CI: 1.42, 1.75), 24% more likely to have dyspnea (RR=1.24; 95% CI: 1.08, 1.41), 45% more likely to be admitted to ICU (RR=1.45; 95% CI: 1.26, 1.67), and 37% more likely to die from to COVID-19 (RR=1.37; 95% CI: 1.30, 1.45) than HIV negative patients.
    Conclusion: HIV/AIDS coinfection with COVID 19 increased the risk of fever, dyspnea, ICU admission, and mortality.
    MeSH term(s) COVID-19 ; Dyspnea/complications ; HIV Infections/drug therapy ; HIV Infections/epidemiology ; Humans ; Pandemics ; SARS-CoV-2
    Language English
    Publishing date 2022-06-20
    Publishing country Canada
    Document type Journal Article ; Meta-Analysis
    ZDB-ID 1422972-9
    ISSN 1482-1826 ; 1482-1826
    ISSN (online) 1482-1826
    ISSN 1482-1826
    DOI 10.18433/jpps32831
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article ; Online: The efficacy and effectiveness of COVID-19 vaccines around the world: a mini-review and meta-analysis.

    Soheili, Marzieh / Khateri, Sorour / Moradpour, Farhad / Mohammadzedeh, Pardis / Zareie, Mostafa / Mortazavi, Seyede Maryam Mahdavi / Manifar, Sima / Kohan, Hamed Gilzad / Moradi, Yousef

    Annals of clinical microbiology and antimicrobials

    2023  Volume 22, Issue 1, Page(s) 42

    Abstract: Objectives: This meta-analysis evaluated the Efficacy and Effectiveness of several COVID-19 vaccines, including AstraZeneca, Pfizer, Moderna, Bharat, and Johnson & Johnson, to better estimate their immunogenicity, benefits, or side effects.: Methods: ...

    Abstract Objectives: This meta-analysis evaluated the Efficacy and Effectiveness of several COVID-19 vaccines, including AstraZeneca, Pfizer, Moderna, Bharat, and Johnson & Johnson, to better estimate their immunogenicity, benefits, or side effects.
    Methods: Studies reporting the Efficacy and Effectiveness of COVID-19 vaccines from November 2020 to April 2022 were included. The pooled Effectiveness/Efficacy with a 95% confidence interval (95% CI) with Metaprop order was calculated. The results were presented in forest plots. Predefined subgroup analyses and sensitivity analyses were also performed.
    Results: A total of twenty articles were included in this meta-analysis. After the first dose of the vaccine, the total effectiveness of all COVID-19 vaccines in our study was 71% (95% CI 0.65, 0.78). The total effectiveness of vaccines after the second dose was 91% (95% CI 0.88, 0.94)). The total efficacy of vaccines after the first and second doses was 81% (95% CI 0.70, 0.91) and 71% (95% CI 0.62, 0.79), respectively. The effectiveness of the Moderna vaccine after the first and second dose was the highest among other studied vaccines ((74% (95% CI, 0.65, 0.83) and 93% (95% CI, 0.89, 0.97), respectively). The highest first dose overall effectiveness of the studied vaccines was against the Gamma variant (74% (95% CI, 0.73, 0.75)), and the highest effectiveness after the second dose was observed against the Beta variant (96% (95% CI, 0.96, 0.96)). The Efficacy for AstraZeneca and Pfizer vaccines after the first dose was 78% (95% CI, 0.62, 0.95) and 84% (95% CI, 0.77, 0.92), respectively. The second dose Efficacy for AstraZeneca, Pfizer, and Bharat was 67% (95% CI, 0.54, 0.80), 93% (95% CI, 0.85, 1.00), and 71% (95% CI, 0.61, 0.82), respectively. The overall efficacy of first and second dose vaccination against the Alfa variant was 84% (95% CI, 0.84, 0.84) and 77% (95% CI, 0.57, 0.97), respectively, the highest among other variants.
    Conclusion: mRNA-based vaccines against COVID-19 showed the highest total efficacy and effectiveness than other vaccines. In general, administering the second dose produced a more reliable response and higher effectiveness than a single dose.
    MeSH term(s) Humans ; COVID-19/prevention & control ; COVID-19 Vaccines/adverse effects ; COVID-19 Vaccines/therapeutic use ; SARS-CoV-2
    Chemical Substances COVID-19 Vaccines
    Language English
    Publishing date 2023-05-19
    Publishing country England
    Document type Review ; Meta-Analysis ; Journal Article
    ZDB-ID 2097873-X
    ISSN 1476-0711 ; 1476-0711
    ISSN (online) 1476-0711
    ISSN 1476-0711
    DOI 10.1186/s12941-023-00594-y
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article: In Vitro Permeability, Irritability, and Release Evaluation of Commonly Used Topical Diclofenac Gel Preparations (1%, 5%, and 10%).

    Kohan, Hamed Gilzad / Baker, David M / Sani, Shabnam / Bielecki-Wilken, Kathleen A / Ramirez, Alfonso

    International journal of pharmaceutical compounding

    2021  Volume 25, Issue 2, Page(s) 146–155

    Abstract: Recently, there has been an increase in the use of compounded topical pain preparations, raising concerns that clinicians and patients may not be aware of the potential safety risks. Topical diclofenac is one of the most widely used pain medications, ... ...

    Abstract Recently, there has been an increase in the use of compounded topical pain preparations, raising concerns that clinicians and patients may not be aware of the potential safety risks. Topical diclofenac is one of the most widely used pain medications, often used for joint ailments such as osteoarthritis and other musculoskeletal pain. Systemic exposure to diclofenac has a dose-related risk for gastrointestinal, cardiovascular, and renal adverse events, particularly in elderly patients. Topical diclofenac preparations are frequently compounded in pharmacies at the concentrations of 1% to 10% (or higher) with or without other active ingredients such as camphor. Considering the significantly higher strengths of the compounded preparations as compared to the commercially available products (1% to 3%) and the frequency of application (sometimes up to six times a day), concerns arise as to the levels of absorption with these formulations and their potential toxicity. The objective of this initial study was formulated in an attempt to shed light on safety concerns of topical diclofenac preparations. A study was designed to evaluate the in vitro release, irritability, and permeability of three different concentrations of compounded diclofenac gels (1%, 5%, and 10%) in PLO GEL MEDIFLO and VersaPro Gel bases. Using MatTek's EpiDerm system, skin irritability and the in vitro permeation of compounded diclofenac gels were evaluated. Additionally, the in vitro release profile, drug content, content uniformity, and physical properties of the compounded gels (pH, homogeneity) were assessed. In all cases, the drug content, content uniformity, physical properties, and preparation stability during the recommended beyond-use dating (90 days) were acceptable. The release profiles of all tested preparations followed the Higuchi model. The in vitro skin irritation evaluation of the tested formulations indicated no irritant preparation. The permeability assessment of the formulated gels revealed that there is a correlation between drug release and percutaneous absorption. VersaPro Gelbased preparations, which showed a lower percentage of drug release over the experiment time, showed a significantly lower average flux at steady-state and the average percentage of absorbed dose after 24 hours. The percentage absorption (%abs) from different formulations ranged from 11.18% to 19.6% depending on the gel base. The permeability coefficient, kp, (cm/hr) ranged from 0.019 to 0.037, and the average flux (µg/cm2/hr) ranged from 8.7 to 103 depending on the gel base and the diclofenac concentration. Based on our findings and previously reported data, the possibility exists that higher diclofenac concentrations in compounded topical preparations may lead to significantly higher blood concentrations as compared to commercially available products, which in turn may also lead to serious side effects. Accordingly, there is a need for clinical studies to evaluate the safety of compounded diclofenac preparations with higher diclofenac contents than United States Food and Drug Administrationapproved formulations.
    MeSH term(s) Administration, Topical ; Aged ; Anti-Inflammatory Agents, Non-Steroidal/adverse effects ; Diclofenac/adverse effects ; Gels/metabolism ; Humans ; Permeability ; Skin/metabolism ; Skin Absorption
    Chemical Substances Anti-Inflammatory Agents, Non-Steroidal ; Gels ; Diclofenac (144O8QL0L1)
    Language English
    Publishing date 2021-04-02
    Publishing country United States
    Document type Journal Article
    ISSN 1092-4221
    ISSN 1092-4221
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: Time and concentration dependency of P-gp, MRP1 and MRP5 induction in response to gemcitabine uptake in Capan-2 pancreatic cancer cells.

    Kohan, Hamed Gilzad / Boroujerdi, Mehdi

    Xenobiotica; the fate of foreign compounds in biological systems

    2015  Volume 45, Issue 7, Page(s) 642–652

    Abstract: 1. Influx and efflux proteins play a major role in the overall uptake and efficacy of chemotherapeutic agents and cellular chemo-resistance. 2. The present study investigated the time course and dose dependency of the induction of three efflux proteins, ... ...

    Abstract 1. Influx and efflux proteins play a major role in the overall uptake and efficacy of chemotherapeutic agents and cellular chemo-resistance. 2. The present study investigated the time course and dose dependency of the induction of three efflux proteins, P-gp, MRP1 and MRP5, in response to gemcitabine exposure in Capan-2 pancreatic cancer cell line at transcriptional and translational levels. The influence of exposure on the influx protein (ENT1), the net cellular uptake of the gemcitabine, the overall ATPase activity and the cell death rate were also measured. 3. The time course of the expression exhibited an initial rise, toward a plateau level. The estimated Km and Vmax confirmed that MRP5 and to a lesser extent MRP1 are the prominent proteins for efflux of gemcitabine. Both mRNA and protein expression demonstrated the time and concentration dependency of the induction; and the elevated ATPase activity validated that the induced efflux proteins are functionally active. 4. The results of the study revealed that the efficacy window of gemcitabine as it relates to the function of the efflux proteins is concentration and temporal dependent and is well correlated to the first 60 min of exposure.
    MeSH term(s) ATP-Binding Cassette, Sub-Family B, Member 1/metabolism ; Adenosine Triphosphatases/metabolism ; Blotting, Western ; Cell Death/drug effects ; Cell Line, Tumor ; Cell Membrane/enzymology ; Cell Survival/drug effects ; Chromatography, High Pressure Liquid ; Deoxycytidine/analogs & derivatives ; Deoxycytidine/pharmacology ; Gene Expression Regulation, Neoplastic/drug effects ; Humans ; Kinetics ; Multidrug Resistance-Associated Proteins/metabolism ; Pancreatic Neoplasms/metabolism ; Pancreatic Neoplasms/pathology ; RNA, Messenger/genetics ; RNA, Messenger/metabolism ; Real-Time Polymerase Chain Reaction ; Time Factors
    Chemical Substances ABCC5 protein, human ; ATP-Binding Cassette, Sub-Family B, Member 1 ; Multidrug Resistance-Associated Proteins ; RNA, Messenger ; Deoxycytidine (0W860991D6) ; gemcitabine (B76N6SBZ8R) ; Adenosine Triphosphatases (EC 3.6.1.-) ; multidrug resistance-associated protein 1 (Y49M64GZ4Q)
    Language English
    Publishing date 2015
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 120287-x
    ISSN 1366-5928 ; 0049-8254
    ISSN (online) 1366-5928
    ISSN 0049-8254
    DOI 10.3109/00498254.2014.1001809
    Database MEDical Literature Analysis and Retrieval System OnLINE

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