Tropical Journal of Pharmaceutical Research

Anticancer screening and GC-MS metabolite profiling of endemic southwest Florida flora: Evaluating the therapeutic potential of three tropical species against Glioblastoma Multiforme

2026-07-11T06:42:24+00:00

Purpose: To examine the cytotoxic effects of crude polar extracts from Byrsonima lucida, Pinus elliottii, and Ulmus alata against LN-229 glioblastoma cells.

Methods: Cytotoxicity was evaluated by MTT assay, while differential gene and protein expression of apoptosis-related markers were assessed by RT-qPCR and ELISA, respectively. Phytochemical constituents were characterized by gas chromatography-mass spectrometry (GC-MS) analysis.

Results: Byrsonima lucida demonstrated the strongest effects, reducing cell viability to 19 % at 48 h, with 4-fold upregulation of CASP3 and 278-fold increase in BAX expression. Pinus elliottii suppressed CASP3 by 23-fold despite inducing cytotoxicity mediated by 32-fold BAX upregulation, suggesting caspase-independent death mechanisms. ELISA confirmed 33 % CASP3 upregulation in B. lucida-treated cells and 58 % suppression in P. elliottii-treated cells. Ulmus alata showed minimal cytotoxicity against LN-229 cells but accelerated wound closure in healthy human astrocytes. GC-MS identified phytochemical profiles distinct to each species, including aziridine derivatives in B. lucida, and topotecan-like compounds in U. alata.

Conclusion: B. lucida and P. elliottii extracts induce glioblastoma cell death through distinct mechanisms, caspase-dependent apoptosis and caspase-independent pathways, respectively, while U. alata shows potential for tissue repair applications.

Development of mucoadhesive solid lipid nanoparticles for enhanced oral bioavailability and antimalarial efficacy of artemether/lumefantrine

2026-07-11T09:38:59+00:00

Purpose: To report the development of mucoadhesive solid lipid nanoparticles (SLNs) to enhance oral bioavailability and antimalarial efficacy of artemether and lumefantrine.

Methods: The SLNs were prepared via hot emulsion–ultrasonication using a lipid matrix composed of dika fat (Irvingia gabonensis) and Phospholipon® 90H. Chitosan coating was applied to confer mucoadhesive properties and prolong gastrointestinal residence time. Fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC) were employed to determine the drug-excipient interaction and thermal properties of the nanoparticles, respectively. Antimalarial properties of the formulated nanoparticles were carried out in vivo using Plasmodium berghei-infected Wistar albino mice.

Results: The SLNs, formulated as individual and co-drug-loaded systems, achieved high encapsulation efficiencies (> 99 % for artemether; > 92 % for lumefantrine). Co-loading improved drug release compared to single-drug SLNs (artemether: 86.2 vs. 58.7 %; lumefantrine: 74.8 vs. 63.8 % over 6 – 8 h). The nanoparticles were spherical, with mean diameters 91.3 – 140.1 nm and polydispersity indices < 0.42. Fourier transform infrared spectroscopy and DSC analyses confirmed drug–excipient compatibility and stable incorporation of both drugs within the lipid matrix. In vivo evaluation in Plasmodium berghei-infected Wistar albino mice revealed a dose-dependent, statistically significant (p < 0.05) reduction in parasitemia for the SLN formulations compared to control.

Conclusion: Chitosan-coated SLNs offer a promising platform for oral delivery of artemether-lumefantrine, with potential to overcome current limitations in bioavailability and therapeutic consistency in malaria treatment.

Preparation and in vitro - ex vivo evaluation of ticagrelor solid lipid nanoparticles

2026-07-11T09:49:01+00:00

Purpose: To investigate the physicochemical properties of Ticagrelor solid lipid nanoparticles (TCG-SLN).

Methods: Formulations were developed based on a 3-level factorial design and subsequently produced using the microemulsion technique. Quality-by-design technique was used to establish correlations between formulation parameters (surfactant ratio, surfactant type, and sonication time) and key quality attributes such as particle size (PS), polydispersity index (PDI), and entrapment efficiency (EE %).

Results: Optimized TCG-SLN showed PS of 67 nm, PDI of 0.165, and EE of 87.5 % with 88 % drug release achieved in 24 h in a controlled manner. Ex vivo permeability showed a 3.3-fold increase in TCG-SLNs permeation compared to Ticagrelor suspension. Scanning electron microscope (SEM), Fourier Transform Infrared spectroscopy (FTIR), and Powder X-ray Diffraction (PXRD) showed that Ticagrelor was effectively encapsulated in the nanoparticulate system, having a non-aggregated, spherical surface with no distinct change in functional groups.

Conclusion: This study shows that TCG-SLN appears as non-aggregated, spherical SLNs with various sizes, exhibits a biphasic release profile, exhibits high intestinal permeability, restores histological structure resembling normal morphology, with short-term stability.

Effect of superdisintegrant type and concentration on dissolution behaviour of Ondansetron orodispersible tablets

2026-07-11T09:52:28+00:00

Purpose: To investigate the effect of various superdisintegrants on disintegration time and early-phase dissolution in ondansetron hydrochloride orodispersible tablets (ODTs).

Methods: A total of 12 formulations were prepared by direct compression using a 3×4 full factorial design. Crospovidone (CPV), sodium starch glycolate (SSG), and croscarmellose sodium (CCS) were each tested at 2, 4, 6, and 8 % w/w. Primary responses were disintegration time, 5-minute drug release, dissolution similarity (f2), and Korsmeyer–Peppas exponent (n).

Results: All blends had acceptable flow properties. At 8 % w/w, CPV released 77.2 % within 5 min compared to SSG (p < 0.01), f2 = 45.3 between CPV and SSG indicated dissimilar profiles, and f2 = 90.8 between SSG and CCS confirmed equivalent swelling-polymer behaviour. Korsmeyer–Peppas modelling gave n = 0.33 for CPV (Fickian diffusion) and n = 0.45, 0.44 for SSG and CCS, respectively, consistent with partial gel-layer resistance. Korsmeyer–Peppas rate constant showed kKP = 40.09 min-n for CPV compared to 7.13 min-n and 28.50 min-n for SSG and CCS, respectively. Furthermore, CPV produced faster early drug release compared to SSG and CCS at all concentrations.

Conclusion: Crospovidone shows significantly superior early-phase dissolution at all concentrations compared with SSG and CCS

In vitro assessment of the antiproliferative effects of Iraqi Euryops pectinatus ethyl acetate extract on MDA-MB-231 breast cancer cells

2026-07-11T09:58:26+00:00

Purpose: To investigate the antiproliferative activity of ethyl acetate extract of Iraqi Euryops pectinatus on MDA-MB-231 human breast cancer cells.

Methods: The dried plant material was extracted by maceration with solvents of increasing polarity. The ethyl acetate extract was subjected to RP-HPLC for phytochemical profiling. The antiproliferative activity of the extract was assessed by MTT assay on MDA-MB-231 breast cancer cells.

Results: Several phenolic and flavonoid compounds such as quercetin, apigenin, rutin, rosmarinic acid, caffeic acid and naringenin were present. Cytotoxic activity of the ethyl acetate extract was concentration-dependent against MDA-MB-231 cells with an IC50 value of approximately 2023 µg/mL. Cell viability decreased significantly with increasing extract concentrations, indicating moderate antiproliferative activity (p < 0.05). Observed activity may be associated with combined or synergistic effects of the identified phenolic and flavonoid constituents.

Conclusion: Euryops pectinatus significantly exhibits cytotoxic activity against MDA-MB-231 breast cancer cells in a concentration-dependent manner, attributed to the synergistic effects of the phytoconstituents.

Multidrug resistance and biofilm formation in methicillin-resistant Staphylococcus aureus from pregnant women attending antenatal clinic with asymptomatic bacteriuria in Rivers State, Nigeria

2026-07-11T10:03:24+00:00

Purpose: To determine the prevalence of asymptomatic bacteriuria (ASB), methicillin-resistant Staphylococcus aureus (MRSA), and biofilm-forming S. aureus among pregnant women seeking antenatal care services in Rivers State, Nigeria.

Methods: A cross-sectional study was carried out at three tertiary hospitals, namely, the University of Port Harcourt Teaching Hospital (UPTH), Rivers State University Teaching Hospital (RSUTH), and Madonna University Teaching Hospital (MUTH), spanning from January 2024 to March 2024. Midstream urine samples of 10mL were collected from 423 consenting pregnant women and analysed microbiologically for bacterial isolation. Bacterial isolates were identified using standard biochemical methods, and MRSA detection was performed via disk diffusion. Analysis, including antibiotic susceptibility and biofilm production, was also evaluated.

Results: A high prevalence of bacteriuria (75.29 %) was recorded, with RSUTH recording the highest occurrence (43.70 %). MRSA prevalence varied across facilities, with MUTH showing the highest methicillin resistance (68 %). All bacterial isolates exhibited multidrug resistance (MDR), particularly against cephalosporins and fluoroquinolones. Biofilm production was detected in 2.5, 13.6, and 20 % of isolates from UPTH, RSUTH, and MUTH, respectively.

Conclusion: There was a high prevalence of bacteriuria and MRSA across the health facilities in Rivers State. This is a critical public health concern, and calls for targeted antimicrobial stewardship programmes in antenatal care.

Synthesis, characterization, molecular docking and pharmacokinetics of new pyrimidine carboxylate derivatives as potent VEGFR inhibitors

2026-07-08T13:27:41+00:00

Purpose: To investigate the strategic design and synthesis of three new pyrimidine carboxylate derivatives aimed at inhibiting VEGFR signaling pathways to suppress tumor growth.

Methods: A set of 3 new pyrimidine carboxylate derivatives was successfully synthesized via optimized chemical routes. Structural integrity of the synthesized compounds was characterized using advanced spectroscopic techniques, including FT-IR, 1H-NMR, and 13C-NMR. Furthermore, multidimensional in silico investigations were conducted to evaluate therapeutic potential.

Results: According to the simulation of molecular docking, the three derivatives demonstrated a high potential for bonding in the vascular endothelial growth factor receptor (VEGFR) active site forming stable complex structures through a series of key hydrogen bond and hydrophobic interactions between important amino acid residues. Additionally, complete ADMET profiling indicated that the three compounds have excellent pharmacokinetic profiles and high oral bioavailability.

Conclusion: This study shows that the synthesized pyrimidine carboxylates bind effectively with VEGFR active site, demonstrate favourable pharmacokinetic properties and high oral bioavailability. Keywords:

Computational docking study of naproxen binding to COX-2 (6COX) using AutoDock and visualization tools

2026-07-11T10:27:16+00:00

Purpose: To investigate the molecular interaction of Naproxen and cyclooxygenase (COX) using a docking approach.

Methods: Naproxen structure was built and energy minimized in HyperChem to attain its stable conformation. The COX receptor (PDB ID: 6COX) was prepared by stripping water molecules and co-crystal ligands, adding polar hydrogens and assigning charge prior to performing molecular docking. AutoDock Vina was used to dock Naproxen to predict its orientation within the COX active site.

Results: The docking yielded five binding modes with the best-ranked pose having a binding affinity of −7.643 kcal/mol, which indicates favorable binding. Visualization by PyMOL indicates that Naproxen fits well inside the COX binding pocket, where the aromatic core is buried deep in the hydrophobic channel, while the carboxylic group is directed toward the pocket entrance, supporting stabilizing interactions.

Conclusion: Naproxen binds within the COX active site with a predicted binding affinity of −7.643 kcal/mol. The ligand is stabilized by hydrophobic interactions and hydrogen bonding.

Behavioural and oxidative effects of Melissa officinalis leaf ethanol extract in a valproic acid-induced rat model of autism spectrum disorder

2026-07-11T11:04:48+00:00

Purpose: To determine the effect of ethanolic leaf extract of Melissa officinalis on the behavioral and oxidative stress parameters in a prenatal valproic acid (VPA) induced rat model of autism spectrum disorder.

Methods: Pregnant Wistar rats were administered VPA (600 mg/kg, subcutaneously) or saline on gestational day 12.5. Control dams (saline group) received an equivalent volume of 0.9 % normal saline subcutaneously on the same gestational day. The male offspring were then administered 100 mg/kg of M. officinalis extract orally or vehicle (tap water) daily on postnatal days 35 - 82. Social behavior assessment was performed on postnatal day 1, and hippocampal biochemical analysis was conducted on the 10th day across four groups (n = 5 rats per group).

Results: Gas chromatography-mass spectrometry (GC-MS) phytochemical analysis revealed the presence of eight major constituents, with α-terpineol being dominant (29.898 %). Prenatal exposure to VPA resulted in severe social deficit with a negative sociability index (-0.286 ± 0.225 vs. 0.36 ± 0.116 in controls) and social novelty index (-0.33 ± 0.295 vs. 0.841 ± 0.089 in controls). This social deficit was completely restored by M. officinalis treatment (p < 0.05). Valproic acid administration reduced superoxide dismutase activity by 41.3 % and malondialdehyde by 70.3 % compared to control, thereby resulting in severe oxidative stress in the hippocampus due to reduction of glutathione levels by 17.4 %. This process was also reversed by the administration of M. officinalis.

Conclusion: Melissa officinalis extract reverses core autism-like social behavioral impairments and exhibits significant antioxidant and neuroprotective effects. This study justifies its ethnomedical therapeutic application.

Evaluation of in vivo toxicity of selected Nigerian medicinal plants used against viral diseases

2026-07-11T10:36:57+00:00

Purpose: To evaluate the subchronic toxicity of four plants frequently used in Nigerian ethnomedicine to treat various viral infections.

Methods: Andrographis paniculata, Artemisia annua, Annona muricata, and Bryophyllum pinnatum extracts were assessed for their subchronic toxic effect in albino rats (Sprague-Dawley strain). Each extract was administered orally at 100, 200, and 400 mg/kg body weight once daily for 28 days, and the biochemical and haematological parameters of the animals were evaluated. The average body weights of the rats were taken before and after the treatment, after which they were sacrificed under chloroform anaesthesia. Blood samples were collected through cardiac puncture and were used to assess for toxicity markers (lipid profile, liver and renal function parameters, and haematological indices).

Results: The sub-chronic administration of these plants, especially Annona muricata and Bryophyllum pinnatum, caused a significant decrease in body weight, an increase in blood glucose and liver enzymes (Alkaline phosphatase and Alanine aminotransferase), and a decrease in hematocrit (HCT) and platelet (PLT) count (p < 0.05). A. paniculata extract was shown to tend to cause dislipidaemia due to the significant increase in serum levels of total cholesterol and low-density lipoprotein cholesterol (p < 0.05).

Conclusion: The findings from the study show that the extracts altered toxicological indices in a dose-dependent manner. Hence, caution is needed in the long-term use of these plant extracts.

Pharmacognostic assessments and phytochemical mapping of ribwort plantain tissues: Integrated findings from ED-XRF, NMR and hyphenated chromatographic analyses

2026-07-11T10:47:50+00:00

Purpose: To conduct a phytochemical mapping of ribwort plantain organs, with emphasis on organ-specific distribution of important bioactive compounds.

Methods: Pharmacognostical and phytochemical characteristics of the plant parts were profiled using preliminary phytochemical screening, Energy Dispersive X-ray Fluorescence (ED-XRF), Gas Chromatography – Mass Spectrometry (GC-MS), Thin Layer Chromatography (TLC), High Performance Thin Layer Chromatography (HPTLC), Liquid Chromatography – Mass Spectrometry (LC-MS) and Nuclear Magnetic Resonance (NMR).

Results: Preliminary test and GC-MS analysis of the plant revealed various phytochemical constituents of the plant parts. The ED-XRF findings revealed a high calcium level with the absence of toxic heavy elements (Pb, Cd, As). The LC-ESI-MS detected isolated phytochemicals as Na+ adducts, while NMR elucidated their structures.

Conclusion: The study revealed isolated accumulation of active metabolites, with flowers and roots demonstrating higher levels of catalpol and aucubin, respectively, while seeds showed the lowest concentration of acteoside.

Clinical efficacy of tamsulosin and tadalafil in distal urethral stone passage: A randomized clinical trial

2026-07-11T10:55:33+00:00

Abstract:
Purpose: To investigate the efficacy of tamsulosin in combination with tadalafil compared to tamsulosin alone in distal ureteral stones.

Methods: A total of 80 adult patients with single distal ureteral stones (5–12 mm) were included in this randomized open-label study. The patients were randomly and equally assigned into study and control groups. Study group (n = 40) received tamsulosin (0.4 mg) plus tadalafil (5 mg) daily, and control group received (n = 40) received tamsulosin (0.4 mg) alone. Follow-up was done for 20 days, and clinical parameters such as stone expulsion rate, time of expulsion, frequency of pain episodes, analgesic requirements, and side effects were compared between both groups. Categorical data were compared using chi-square test. Measurement data were compared using the independent sample t-test. P < 0.05 was considered statistically significant

Results: Stone expulsion rate was significantly higher, and mean stone expulsion time was significantly shorter in study group compared to control (p < 0.05). Furthermore, patients in study group experienced significantly fewer pain episodes and required analgesics less frequently (p < 0.05). Adverse effects were milder with no significant difference between the groups (p > 0.05), with no major complications.

Conclusion: Tadalafil in combination with tamsulosin significantly increases expulsion rate, accelerates stone expulsion, reduces pain and analgesic use in patients with distal ureteral calculi without any significant increase in side effects.

Healthcare service quality and utilisation patterns among university students: A SERVQUAL-based assessment

2026-07-11T11:20:00+00:00

Purpose: To examine the perception of Obafemi Awolowo University (OAU) undergraduate students about service quality at the institution's Health Centre and determine if their perception had an effect on their use of healthcare services.

Methods: The study adopted a cross-sectional mixed-methods design. For quantitative determinations, a SERVQUAL-based survey was administered to 1,698 undergraduates. The instrument covered the five core service quality dimensions: tangibles, reliability, responsiveness, assurance, and empathy. A focus group discussion of 14 students was used to obtain qualitative data. Quantitative data were analysed using factor analysis and multiple linear regression; qualitative transcripts were analysed thematically to further explain the survey findings.

Results: The results showed that only 527 (31.1 %) had accessed services within the preceding six months, even though 1148 (67.6 %) of respondents reported being registered with the Health Centre. The perceptions of service quality overall were moderately positive (mean = 3.17 ± 0.95); the results also revealed that expectations consistently exceeded experiences with a negative SERVQUAL gap (−1.19 ± 1.13). Responsiveness showed an inverse relationship with service utilisation, while perceived reliability and empathy were positively associated. A little over half (53.6 %) of the observed variance was accounted for by these underlying factors. The focus group discussion identified unfavourable staff attitudes, long waiting times, and procedural delays as key deterrents to healthcare utilisation.

Conclusion: Student confidence and utilisation of university health services can be increased by improving responsiveness, reliability, and interpersonal aspects of care.

Impact of using metformin alone or with sitagliptin on diabetes management and their association with cardiovascular and renal outcomes

2026-07-11T11:34:28+00:00

Purpose: To investigate the effect of metformin monotherapy against sitagliptin-metformin combination on blood pressure, glucose metabolism, renal function, and lipid profile.

Methods: Three separate groups of 150 participants each were assigned at random and equally. Group 1 served as the control. Group 2 received metformin, then group 3 received sitagliptin with metformin. Biochemical and physiological parameters, including HbA1c, fasting blood sugar (FBS), blood pressure, high-sensitivity cardiac troponin (hs-cTn), lipid profile, blood urea (BU), and serum creatinine (Cr), were measured and recorded.

Results: Groups 1 and 2 showed significantly higher HbA1c and FBS related to control group (p < 0.05), although group 2 had higher FBS levels. Group 2 had significantly higher systolic blood pressure and high-sensitivity cardiac troponin (hs-cTn) in comparison to control (p < 0.05), whereas group 2 demonstrated lower high-sensitivity cardiac troponin (hs-cTn) and systolic pressure values. Despite total cholesterol was relatively higher in group 1, the lipid profile assessment revealed just modest, non-significant variations. In both groups 1 and 2, renal function parameters exhibited considerably diminished BU and Cr, suggesting possible nephroprotective effects.

Conclusion: In comparison to metformin alone, a combination of sitagliptin and metformin optimises the regulation of cardiovascular and renal indicators.

Keratin in drug delivery: A narrative review of sources, processing techniques, formulation strategies, and biomedical applications

2026-07-11T11:41:17+00:00

Keratin is a naturally occurring fibrous structural protein that has attracted considerable attention as a biomaterial due to its excellent biocompatibility, biodegradability, low immunogenicity, and intrinsic cell-binding properties. These characteristics designate keratin as a promising candidate for biomedical and pharmaceutical applications, particularly in drug delivery systems. This study investigated keratin molecule, physicochemical properties suitable for drug delivery, some keratin-based formulations from 2015 to 2025, and applications of keratin. The study also presented an array of extraction methods comparing their yield, feasibility, and disadvantages. Furthermore, future perspectives and research opportunities for safer methods, hybrid systems for targeted therapy, stimuli-responsive systems, gene delivery systems, bioinks, and personalized medicine were also hypothesized. The review also presented some challenges and limitations, including breaking the extensive disulfide linkages using toxic, non-eco-friendly chemicals; variability in amino acid composition among different keratin sources, resulting in difficulty in standardization and reproducibility; and limited in vivo studies, which have limited the clinical application of the developed systems. Future research should focus on developing greener extraction technologies, standardizing keratin-based formulations, and conducting comprehensive preclinical and clinical evaluations to facilitate its successful integration into pharmaceutical and biomedical practice.