Volume: 20  Issue: 3 - 2023
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RESEARCH ARTICLE
1.Thermoreversible gel formulation for intranasal delivery of salmon calcitonin and comparison studies of in vivo bioavailability.
Abdullah Levent Alparslan, Gülbeyaz Yıldız Türkyılmaz, LEYLA DIDEM KOZACI, Ercument Karasulu
Pages 127 - 140
INTRODUCTION: The reason for studying thermoreversible gel form is to arrange viscosity of formulations for a reversible adequate fluidity in different temperatures. This situation may facilitate use of drug as spray and increase bioadhesive ability to mucosa
METHODS: In the current study, we developed original thermoreversible nasal solgel formulations of salmon calcitonin (sCT). The solgel has been compared with the commercial intranasal spray. same amount of commercial and solgel dosages were sprayed into the noses of the rabbits. Blood samples collected from the ear veins of rabbits and analyzed by EIA.
RESULTS: Using AUC0→tlast in primary pharmacokinetic data, the absolute bioavailability of the formulation at pH: 4 was found to be comparable to that of a commercial product. The absolute bioavailability of the commercial product was measured as 1.88 based on the Cmax. Cmax of the optimum formulation pH: 4 was 0.99 and the relative bioavailability was 53.3%.
DISCUSSION AND CONCLUSION: It is thought that the adhered formulation to the nasal mucosa releases sCT slowly and less. In vivo pharmacokinetic data of solgel formulation with pH: 3 showed significantly higher Vd parameter than commercial product (111167 > 35408). Such being this case the affinity of drug can be more to tissues rather than blood plasma in solgel formulation.
Abstract

2.Preparation and Characterization Studies of Dorzolamide Loaded Ophthalmic Implants for the Treatment of Glaucoma
Samet Özdemir, Egemen Çakırlı, Bilge Sürücü, Cemre İrem Aygüler, Burcu Üner, Ali RizaCenk Celebi
Pages 149 - 156
INTRODUCTION: This study aimed to construct dorzolamide loaded ophthalmic implants for extended drug delivery and increased drug retention
METHODS: Carboxymethyl cellulose and Chitosan were used to formulate the ophthalmic implants. The implants were prepared by solvent casting technique in existence of polyethylene glycol 6000 as plasticizer. Physiochemical characterization studies including mechanical characteristics (tensile strength, elongation at break, and Young’s modulus), bioadhesion studies, in vitro and ex vivo drug release studies were conducted.
RESULTS: Tensile strength of drug loaded ophthalmic implants were 10.70 and 11.68 MPa respectively. Elongation at break of Carboxymethyl cellulose and Chitosan implants were 62.00% and 59.05% respectively. The in vitro release profiles fit into the Higuchi type kinetic model. Ex vivo release study results for both implants were correlated with in vitro release investigations.
DISCUSSION AND CONCLUSION: Carboxymethyl cellulose and Chitosan based implants provide extended drug delivery. Implants were prepared by using carboxymethyl cellulose provide significantly slower in vitro release rate, and the drug retention on ocular surfaces has been increased. Thus, it has been concluded that, dorzolamide loaded carboxymethyl cellulose implants could provide effective treatment for glaucoma.
Abstract

3.HERPUD1, a member of the Endoplasmic Reticulum Protein Quality Control Mechanism, may be a good target for suppressing tumorigenesis in Breast Cancer Cells.
Yalcin Erzurumlu, Yagmur Doganlar, Hatice Kubra Dogan, Deniz Catakli
Pages 157 - 164
INTRODUCTION: Breast cancer is the most frequently diagnosed cancer type in women, and it is the second leading cause of cancer-related death in women. Recent studies highlight the importance of the Endoplasmic reticulum (ER) protein quality control (ERQC) mechanism for the survival of many cancers and it also has been recommended as a good target for the treatment of many cancer types. Homocysteine inducible ER protein with ubiquitin-like domain 1 (HERPUD1) functions as one of the main components of ER-associated degradation (ERAD), which is an ER-resident protein quality mechanism. Today, the association of HERPUD1 with breast carcinogenesis is still not fully understood. Herein, we evaluate the possibility of HERPUD1 as a potential therapeutic target for breast cancer.
METHODS: The effect of HERPUD1 silencing on epithelial-mesenchymal transition, angiogenesis and cell cycle proteins was analyzed by immunoblotting studies. To test the role of HERPUD1 on tumorigenic features, WST-1 based cell proliferation assay, wound-healing assay, 2D colony formation assay and Boyden-Chamber invasion assay were performed in MCF-7 cells. The statistical significance of the differences between the groups was determined by Student t-test.
RESULTS: Our results showed that suppression of HERPUD1 expression led to decreased cell cycle-related protein levels including Cyclin A2, Cyclin B1 and Cyclin E1 in MCF-7 cells. Also, silencing of HERPUD1 was remarkably decreased expression levels of epithelial-mesenchymal transition-related N-cadherin and angiogenesis marker, VEGF-A. Moreover, we determined that significantly decreased the cell proliferation, migration, invasion and colony formation in HERPUD1 silenced MCF-7 cells.
DISCUSSION AND CONCLUSION: HERPUD1 may have the potential to be an effective target for biotechnological and pharmacological targeting strategies to be developed for the treatment of breast cancer.
Abstract

4.Analytical quality by design driven development and validation of an UV-visible spectrophotometric method for quantification of Xanthohumol in bulk and solid lipid nanoparticles
Harish Vancha, Devesh Tewari, Rajesh Kumar, Pilli Govindaiah, Sharfuddin Mohd, Sachin Kumar Singh, Monica Gulati
Pages 165 - 175
INTRODUCTION: Xanthohumol (XH) is a prenylated chalcone available naturally and having diverse pharmacological activities. It has some limitations in the physiological environment like biotransformation, less GIT absorption. To overcome the limitations, we prepared nanoformulations (solid lipid nanoparticles) of XH. Therefore, an analytical method is required for the estimation of XH in the bulk nanoformulations so, we developed and validated QbD based UV-spectrophotometric method as per ICH Q2 (R1) guidelines.
METHODS: The new AQbd based UV-Visible spectrophotometric technique is developed and validated for estimation of xanthohumol in bulk and solid lipid nanoparticles as per ICH guidelines Q2 (R1). The critical method variables (CMVs) are selected based on risk assessment studies. Optimization of method variables was performed by using CCD model.
RESULTS: Multi-regression ANOVA analysis showed R2 value 0.8698 which is nearer to 1 that indicates the model was best fitted. The optimized method by CCD is validated for its linearity, precision, accuracy, repeatability, LOD and LOQ and specificity. All the validated parameters were found to be within the acceptable limits (%RSD<2). The method was linear between 2-12µg/ml concentration with R2 value 0.9981. Method was accurate with % recovery 99.3%-100.1%. The LOD and LOQ was found to be 0.77 and 2.36 μg/mL respectively. The precision investigation was also confirmed the method was precise with %RSD<2.
DISCUSSION AND CONCLUSION: The developed and validated method was applied to estimate the XH in bulk and solid lipid nanoparticles. The developed method was specific to XH which was confined by the specificity study.
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5.Applications of dietary supplements and aromatherapy for prophylactic and treatment purposes during COVID-19 pandemic
Methiye Mancak Karakuş, Ufuk Koca Çalışkan
Pages 176 - 184
INTRODUCTION: The lack of a specific proven treatment for COVID-19 has led individuals to use different treatment options. Although their effects on COVID-19 have not been proven, interest in dietary supplements and aromatherapy has increased during the pandemic period. In this study, usage of dietary supplement and aromatherapy were investigated for COVID-19 among individuals living within the borders of Turkey.
METHODS: This cross-sectional survey study was conducted among 310 indivuduals. The questionnaire was prepared using online Google Forms and communicated to the participants via social media platforms. The data obtained from the study were analyzed with the statistical program.
RESULTS: The analyzes of the survey revealed that participants increased the usage of supplements mostly prophylactic and also for treatment purposes during COVID-19 pandemic, 31.9% individuals declared that they consume herbal tea / product, 38.1% of them use vitamin/mineral supplement (multivitamin‐mineral, vitamins B1,B6,B12,C,D, calcium, coenzymeQ10, iron, magnesium, selenium, zinc) and 18.4% of the indivuduals applied aromatherapy (treatment with essential oils). As a result of the study, the most commonly used supplement was vitamin D, the most commonly consumed tea was green tea and the essential oil was thyme oil, additionally, the most eaten vegetable was garlic. Moreover, other frequently used herbal products were containing ginger, onion as food, peppermint and eucalyptus oils as aromatherapeutics. Participants often reported that they find safe for using the elevated level of herbs or herbal products against COVID-19.
DISCUSSION AND CONCLUSION: Among the individuals participating in this study, it has been observed that the use of dietary supplements has increased during the COVID-19 pandemic period. The study revealed that vitamin D is prominent in self-medication use. Moreover, interest in aromatherapy has increased as well as dietary supplements. Among aromatherapeutics thyme stood out over the applied essential oils.
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6.Development and evaluation of in- situ gel formation for treatment of mouth ulcer
Nikita Harekrishna Gurav, Prerana Shantinath Husukale
Pages 185 - 197
INTRODUCTION: Mouth ulcers are one of the most prevalent conditions that can be caused by a range of circumstances. Many formulations, such as solution, suspension, and ointments, are available commercially. However, because there is no long-term effect, no medication can be regarded to be totally effective in the treatment of mouth ulcers. The use of a bio adhesive method can boost the therapy's efficacy. Because it is easier to administer than prepared gel formulations, the phenomena of sol to gel conversion can be beneficial.
The major goal of this study is to develop and test in situ gels for treating mouth ulcers utilizing choline salicylate and borax as model medicines.
METHODS: Because a thermosensitive polymer was employed in this formulation, the Sol-to-gel change was thermally reversible, and the frequency of administration was reduced by using the mucoadhesive polymer Carbopol. Gelation temperature, pH, gel strength, Spreadability, in vitro mucoadhesion, and in vitro drug release were all measured in the formulations.

RESULTS: The experimental section indicated that viscosity of sols and gel strength was increased with increase in temperature, i. e. gel can be created at site of application owing to body temperature. When Poloxamer 407 was used at a concentration of 14 to 16 percent w/v, the gelling temperature was close to the body temperature (35-38°C), but when here Carbopol 934P was added, the gelling temperature was raised. All formulations had a pH between 5.5 and 6.8, All formulations had viscosities of less than 1000 cps, allowing for simple administration of the formulation to a mouth ulcer.
DISCUSSION AND CONCLUSION: As a result, a correctly developed in-situ gel for oral ulcers can extend the duration spent at the application site and minimize the frequency of administration. These findings show that the created technology is a viable alternative to traditional drug delivery systems and can help patients comply.
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7.A Systematic Review of Healthcare Professionals' Knowledge, Attitudes, and Practices Regarding Adverse Drug Reaction Reporting in Ethiopia
Zelalem Gebretsadik Anbeo, Nurettin Abacioglu
Pages 198 - 209
ADRs (Adverse drug reactions) are a prominent cause of morbidity and mortality, as well as higher healthcare expenditures. Healthcare professionals (HCPs) play a crucial role in ADRs reporting through spontaneous reporting system, but under-reporting is its major limitation. The goal of this study is to evaluate HCPs' knowledge, attitude, and practice (KAP) regarding ADR reporting, as well as the factors that influence reporting, using research papers that are currently available. A literature search was conducted using sources such as PubMed, Scopus, and Google Scholar to find studies that evaluated HCPs' KAP regarding ADR reporting in Ethiopia. A systematic review protocol- PRISMA was used to conduct this review. Demographic factors, sample size, response rate (RR), survey delivery, HCPs working setting, were extracted information from articles. A total of 17 articles included in the systematic review out of 384. The number of HCPs in the included studies ranged from 62 to 708. RR ranges from 76.1% to 100%. The majority of the research included in this evaluation looked at HCPs who worked in hospitals. When pharmacists were compared to other HCPs, they were more likely to report ADRs because they had higher knowledge, attitude, and practice. Lack of understanding, unavailability of reporting forms, uncertainty about the causal relationship between the drug and ADR, and failure to report because the ADR was well-known were among the common hurdles to ADR reporting identified in research. To improve reporting, educational initiatives and continued training in pharmacovigilance (PV) and ADR are frequently recommended considerations. In Ethiopia, there is a pressing need to close the gap in HCP KAP regarding PV and ADR reporting. It is suggested that specific educational interventions based on existing gaps in ADR reporting be developed and integrated into the health education curriculum or provided as in-service training after graduation.
Abstract