Journal of Drug Delivery and Therapeutics (JDDT)
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Formulation, Optimization and Evaluation of Solid Dispersion of Deferasirox Using Factorial Design
Get PDFDeferasirox, an oral iron-chelating agent, is a poorly soluble drug (Biopharmaceutical Classification System class II) having insufficient solubility in physiological fluids resulting in low bioavailability of the drug. The idea behind the present study was to explore the prospects of solid dispersion as a prolific method to enhance the dissolution rate of drug using a water soluble polymer. The solid dispersion was prepared by the solvent evaporation technique using Polyvinyl pyrrolidone with different drug to carrier and solvent ratio. Formulations were characterized through attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC), Powder X-ray diffraction (XRD), and in vitro release studies. A 32 factorial design was implemented to obtain optimum solubility, % yield, and optimization of solid dispersion (SD) also quantitates the influence of PVP on the solubility and dissolution profile. Thedrug-to-carrier and solvent ratio was chosen as independent variable, while %yield, drug content, and saturation solubility were chosen as dependent variables. The results showed that the optimized formulation of SD-DFX was able to significantly enhance its solubility. The SD containing a dispersion of Deferasirox with PVP show an exceptional rise in the solubility. This study describes the development of solid dispersion that significantly improved the solubility and bioavailability of DFX. The FTIR studies indicate the interaction between the drug and polymer. The DSC and XRD analysis indicated that the drug was in an amorphous state when dispersed in the polymer. It is resolved that the SD method significantly improves the solubility and dissolution rate, which could also be exploit for other poorly water soluble drug candidates.
Keywords: Deferasirox , Polyvinyl pyrrolidone, solid dispersion, Factorial design, Solubilit
Advancements In Pharmacotherapy for Hyperlipidemia: A Comprehensive Review of Recent Drug Innovations and Clinical Outcomes
Get PDFHyperlipidemia, characterized by elevated blood lipid levels, significantly contributes to cardiovascular diseases (CVDs), the leading cause of global mortality per the World Health Organization (WHO). Studies reveal a 20-30% increase in coronary heart disease risk for every 1 mmol/L rise in LDL-C levels. While statins are widely used, novel pharmacotherapeutic approaches are necessary for effective hyperlipidemia management and CVD risk reduction. Recent clinical trials demonstrate the efficacy of innovative drugs like proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors in lowering LDL-C levels and reducing adverse cardiovascular events. These findings highlight the potential of new therapies to enhance existing treatments for hyperlipidemia. Additionally, safety evaluations of emerging lipid-lowering agents address concerns about adverse effects and long-term risks. Despite progress, challenges persist in refining treatment strategies and ensuring equitable access to advanced therapies, especially for marginalized populations. Incorporating innovative pharmacotherapies into current approaches offers personalized and efficient hyperlipidemia management. Continued research and interdisciplinary collaborations are vital for advancing our understanding of lipid metabolism and translating scientific discoveries into improved patient outcomes and cardiovascular health. Ongoing innovation and investment in tailored hyperlipidemia therapies are crucial for better outcomes in individuals at risk of CVDs.
Keywords: hyperlipidemia, pcsk9 inhibitors, bempedoic acid, evinacumab, inclisiran mipomersen, volanesorse
Binge drinking and the risks to adolescent health
Get PDFAdolescence is a phase characterized by physical, emotional and social changes that make adolescents more susceptible to risky practices and behaviors. One of these common practices is excessive alcohol consumption, known as “binge drinking”, which causes numerous acute and chronic health problems. This article presents some characteristics observed in adolescent development and the consequences of excessive alcohol consumption for physical and emotional health, and its repercussions on community life.
Keywords: Adolescence, Alcohol, Binge Drinking, Adolescent Healt
Exploring Neuroprotective Botanical Remedies in Neurodegenerative Conditions: A Review
Get PDFNeuroprotection refers to the mechanisms and strategies used to protect the Central Nervous System (CNS) from neuronal injuries caused by neurodegenerative disorders. Neurodegenerative disorders are a type of chronic condition in which parts of the nervous system deteriorate over time, most notably the brain. These disorders have a slow and gradual effect on an individual. Neurodegeneration is a neuropathological condition and brain aging process. The brain pathology of neurodegenerative and cerebrovascular disease is a leading cause of death worldwide, with a death rate of approximately 8% and an incidence rate of approximately 2/1000. It is a major health issue in the twenty-first century. According to researchers, this disease affects over 50 million people worldwide. These disorders primarily affect people over the age of 65, and the World Health Organization predicts that this number will more than double in the next 30 years. Confusion, difficulty thinking, pain, muscle spasms, behavioral changes, paralysis, tremors, balance problems, coordination issues, hunched posture, and fatigue are symptoms of these disorders. These disorders are caused by age, genetics, medical history, habits, routine, and environment. This review article is focused on herbs such as Crocus sativus and Curcuma longa which are very helpful in Neurodegenerative diseases and serve as a resource for future research.
Keywords: Neurodegeneration, Medicinal Herbs, Neuroprotection, Neuroprotective plants, Parkinson, Alzheimer
Immunohistochemical Analysis of Sperm Aquaporin-3 Expression in Men with Varicocele
Get PDFObjective: The primary objective of this study is to detect potential alterations in sperm cells in cases of varicocele using immunohistochemical methods.
Materials and Methods: In this study, semen samples obtained with consent from infertile males aged between 25-40 years were analyzed for the presence of varicocele and other determined factors, and were divided into two groups: a normozoospermic control group and a group diagnosed with varicocele. Direct swim-up techniques were utilized to separate spermatozoa with high motility. Immunohistochemical staining methods were employed to visualize protein expression, and the results were photographed at high magnification for documentation.
Results: This research was conducted on sperm samples collected from males diagnosed with varicocele and from a healthy control group. The findings suggest that the presence of aquaporin-3 protein is associated with low or negative expression in sperm cells in the presence of varicocele. Immunohistochemical analyses have revealed a reduced or absent expression of aquaporin 3 in patients with varicocele compared to healthy individuals.
Conclusion: The results of this study clearly demonstrate the adverse effects of varicocele on the structural and functional integrity of spermatozoa. Given that aquaporin-3 protein is critical for the motility of spermatozoa, the reduced expression or absence of this protein sheds light on the molecular mechanisms of male infertility.
Keywords: Sperm DNA fragmentation, immunohistochemistry, Varicocele, protein expression, male infertility, aquaporin-3
Release profile of encapsulated microparticles based on Landolphia owariensis (Apocynaceae) extract contained in suppositories for the treatment of hemorrhoidal crisis
Get PDFIntroduction: Hemorrhoidal disease is one of the most frequent causes of anal complaints. The general aim of this study was to evaluate the release profile of the encapsulated drug, in order to overcome the limitations of conventional galenic forms, while maintaining their efficacy.
Methods: Determination of the active ingredient contained in Landolphia owariensis extract was carried out by UV-Visible spectrophotometry. Release studies were carried out in a continuous flow cell. The dissolution profile of the suppository containing microparticles was compared to the dissolution profile of suppositories containing the unencapsulated extract and to that of Landolphia owariensis extract-based microparticles.
Results: The percentage of active ingredient released from suppositories containing microparticles and those containing the extract alone was 69.47% and 80.01% respectively. Flavonoid release from suppositories containing microparticles was slower, with a release rate of 6.31µg/mm, slightly close to the release rate of extract based microparticles (7.37µg/mn); in contrast, in vitro flavonoid release from suppositories containing the extract was faster (19.85µg/mm).
Conclusion: Release trials have shown the influence of the sodium alginate matrix system on PA release kinetics. These innovative suppositories will help improve compliance and the treatment of hemorrhoidal crisis.
Keywords: Microparticles, Suppositories, Landolphia owariensis, Hemorrhoids, In vitro releas
Preparation, Characterization and Evaluation of Antioxidant Flavonosomes
Get PDFThe objective of the present study was to prepare flavonosomes loaded with kaempferol and curcumin in order to improve the bioavailability of the flavonoids. The flavonosomes loaded with kaempferol and curcumin were prepared using bulk co-loading method using lecithin as the lipid molecule. The particle size of the flavonosomes was determined using zeta sizer and ranged from 497.3 nm to 167.1 nm. The results indicated that increase the ratio of lipid to extract was able to reduce the particle size of the flavonosomes. The flavonosomes prepared using 4:1 ratio of lipid to flavonoids were found to be rigid, spherical as seen in SEM with smooth regular surface. Sharp and distinct endothermic peaks in DSC revealed the formulation of stable flavonosomes due to molecular interactions between the extract and lecithin. The entrapment efficiency of flavonosome preparation F4 was determined by measurement of the non-entrapped flavonoids and subtracting from the total flavonoids used to obtain the flavonoids entrapped in the formulation. The entrapment efficiency of F4 has been calculated to be 94.12%. The flavonosome F4 was studied for release of the entrapped flavonoids by dialysis method. The amount of flavonoids released at 1, 2, 3, 4, 6, 8, 10 and 12 hours was determined using UV spectrophotometry. After the first hour, the entrapped flavonoids released in a steady manner from the flavonosome depicting and almost complete release (90.52% for kaempferol and 94.67% for curcumin) from the formulation. The flavonosomes were found to be stable under the storage conditions. The best formulation with respect to particle size and anti-inflammatory action was F4 that contained 4:1 ratio of lecithin: flavonoids. DPPH radical scavenging assay was used to determine the antioxidant action of the individual flavonoids and the flavonosome formulation. It was found that the formulation F4 was having higher antioxidant activity in comparison to kaempferol and curcumin. The IC50 of kaempferol, curcumin and flavonosome were found to be 228.20 µg/mL, 175.51 µg/mL and 158.19 µg/mL respectively.
Keywords: Flavonosome, Kaempferol, Curcumin, Bulk co-loading, antioxidan
Isolation and Identification of Bacteria from Electronic devices used by Students and Staffs in Ines Ruhengeri
No full textBackground: Electronic devices have become one of the most essential accessories being used in daily lives including schools. Those devices increase the communication and using them makes learning much easier. Microbial contamination of electronic devices and inanimate surface of electronic equipment at INES-Ruhengeri can have a significant role for transmission of pathogenic bacteria.
Aim: The aim of this study was to isolate and identify bacteria from electronic devices used by students and staffs at INES-Ruhengeri University.
Methodology: This cross-sectional study was done on 40 electronic devices such as computers, microscopes, global positioning system (GPS) and total stations A random sampling method was applied from sterile swab soaked in peptone water solution by the technique of bearing on the surface of the entire devices and then placed in a transport medium. Collected samples were then taken in INES-Ruhengeri Microbiology laboratory for further experiments.
Results: All 40 electronic devices were contaminated with bacteria. The most predominant bacteria isolated from electronic devices was S.aureus (25.9%) followed by Bacillus spp(24.1%), K.pneumonia(12.9%), S.epidermis(12.9%), Micrococcus spp(7.4%), P.aeruginosa(5.5%), E.coli(3.3%), Salmonella spp(3.3%) and Shigella spp(3.3%). Antimicrobial susceptibility pattern of selected antibiotics was performed. Norfloxin was the most sensitive antibiotic on all isolated bacteria. Chloramphenicol antibiotic shown no activity over any of the isolated bacteria, to imply that all bacteria had resistance on it.
Conclusion: This study shown that there is bacterial contamination to all devices and antibiotic susceptibility test shown that some antibiotics were sensitive and resistant to the isolated bacteria
Assessment of haematological parameters in HIV patients attending Kabutare district Hospital
Get PDFBackground: Human Immunodeficiency virus (HIV) infection is characterized by progressive weakening of the immune system attributed to the decrease in the number of circulating CD4+ T-helper cells. This predisposes HIV patients to a variety of opportunistic infections and neoplastic disorders. also lead to defective hematopoiesis and a decrease in cell lineage. Haematological parameters including red blood cells, white blood cells, platelet and hemoglobin are widely used clinical indicators of health and disease.
Aim: The aim of this study was to assess haematological parameters in HIV patients attending Kabutare District hospital.
Methodology: This study was a cross-sectional study conducted to assess haematological parameters in HIV patients attending Kabutare District hospital. Venous blood sample were collected for complete blood count which was determined using sysmex 500i machine automation analyser.
Results: A total of 80 HIV infected patient participated. 7.5% of the study participants were proven to have white blood cells below the normal range as it was below 4.26.25% of patients were found below the normal range of red blood cells. Hemoglobin and hematocrit levels of 35% patients were found to below their normal ranges. 10% of patient were found to have low platelet and 23.5% were found to have low levels of lymphocytes. Association between CD4 counts and hemoglobin levels was significant with p value of 0.000 as it is less than confidence level of 0.05.
Conclusion: This study concluded that haematological parameters are affected by HIV infection and there is association between CD4 counts and hemoglobin concentration levels. I would recommend health practioners to also consider complete blood count as prognostic test of HIV as it is clinical health indicator and diseases.
Keywords: Haematological parameters, Human Immunodeficiency virus, CD4 counts, acquired immunodeficiency syndrome
Clinical and Haematological Study of Hijama-Bi’l-Shart (Wet Cupping) In the Management of Pain
Get PDFBackground: This randomized clinical and haematological study evaluated the effect of Hijama-Bil-Shart (Wet Cupping) on musculoskeletal pain and inflammatory markers in venous and cupped blood.
Materials and Methods: 110 patients with musculoskeletal pain were screened, with 90 diagnosed and included. After 30 subjects were lost to follow-up, 60 completed the study. Participants received 4 weekly sessions of wet cupping therapy over 4 weeks. Pain intensity was measured using VAS and KOOS scores, and inflammatory markers (Serum uric acid & CRP) were assessed in venous and cupped blood.
Results: Pain relief, measured by VAS, showed significant improvement across various musculoskeletal conditions: cervical spondylosis, frozen shoulder, low backache, sciatic pain, knee osteoarthritis, gout, and rheumatoid arthritis. KOOS scores for knee osteoarthritis improved significantly. Serum uric acid levels in venous blood were suggestively insignificant, while CRP levels decreased gradually but were not statistically significant. No adverse effects were reported.
Conclusion: Hijama-Bil-Shart (wet cupping) therapy is effective in relieving musculoskeletal pain and improving quality of life. It shows long-term benefits with sustained pain relief and gradual reduction in CRP levels. However, it is not effective in significantly reducing raised serum uric acid levels.
Keywords: Musculoskeletal pain, Wet cupping, VAS, KOOS, Hijama-Bil-Shart, CR