Browsing by Author "Gathirwa, Jeremiah"

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Antimalarial potential and phytochemical composition of fractions of Lippia kituiensis Vatke (Verbenaceae) growing in Northern Tanzania
(Journal of Medicinal Plants Research, 2020-08-31) Ng’etich, Japheth; Swai, Hulda; Njokah, Joseph; Wachira, Sabina; Koech, Lilian; Gathirwa, Jeremiah
Despite past decades of steady advances in the fight against Malaria, statistics show that the disease is still a threat to human health. Previous successes in the development of antimalarial drugs from medicinal plants have fuelled research in this area. However, antimalarial studies on fractionated extracts from such plants have progressed slowly. This study reports the antimalarial potential of fractions from Lippia kituiensis Vatke, for the first time. Column chromatography was used during fractionation. Antiplasmodial assay against chloroquine-sensitive (D6) and resistant (W2) plasmodium strains were done using hypoxanthine incorporation assay. MTT assay was used to assess the cytotoxicity of fractions against the Vero cell line. Fractions obtained exhibited varied inhibitory concentrations (IC50); with the most efficacious being, Lk-5 (19.45 ± 6.20 μg/ml), Lk-3 (30.43 ± 0.68 μg/ml), Lk-4 (30.82 ± 18.01 μg/ml), and Lk-6 (36.53 ± 14.42 μg/ml) against D6. Generally, lower activity against W2 was obtained with the most active being LK-4 (24.18±2.50 μg/ml), and Lk-5 (24.42±5.95 μg/ml), while chloroquine (positive control) exerted IC50 of 77.86±4.09 ng/ml (W2) and 15.71±6.49 ng/ml (D6). LK-4 was the most cytotoxic showing cytotoxic concentration (CC50), 46.26 μg/ml. When tested in mice, fractions suppressed Plasmodium berghei significantly compared to the negative control with Lk-3 being most efficacious (80.01±1). Due to substantive efficacy, GC-MS done on Lk-3 revealed 8 compounds where three have previously been ascribed to antimalarial activity and other pharmacological effects. This study adds to present knowledge of antimalarial efficacy of L. kituiensis and provides the basis for further work to be done on the isolation of compounds from its extracts.
Chitosan-coated liposomes of Carrisa spinarum extract: synthesis, analysis and anti-pneumococcal potency
(ICE Publishing, 2023-02-16) Rubaka, Clarence; Gathirwa, Jeremiah; Malebo, Hamisi; Swai, Hulda; Sibuyi, Nicole; Hilonga, Askwar; Dube, Admire
In the present study, a chitosan (CS)-coated liposome (LipCsP-Chitosan) nanocarrier was fabricated for the delivery of Carissa spinarum (CsP) polyphenols to improve bioavailability and anti-pneumococcal potential against Klebsiella pneumoniae. LipCsP-Chitosan was synthesized by the ion gelation method and characterized by using a Malvern zetasizer and Fourier Transform Infrared (FTIR); CsP encapsulation and release kinetics were investigated. Anti-pneumococcal activity of the nanoformulations was accessed by agar-well diffusion and microdilution assays. LipCsP-chitosan exhibited a hydrodynamic size and zeta potential of 365.22 ± 0.70 nm and +39.30 ± 0.61 mV, respectively. CsP had an encapsulation efficiency of 81.5%. FTIR analysis revealed the interaction of the liposomes with chitosan and the CsP. A biphasic CsP release profile followed by a sustained release pattern was observed. LiPCsP-Chitosan presented a higher bioaccessibility of polyphenols in the simulated gastric phase (74.1% ± 1.3) than in the simulated intestinal phase (63.32% ± 1.00). LipCsP-chitosan had a relative inhibition zone diameter of 84.33% ± 2.51 when compared to CsP. At minimum inhibition concentration of 31.25 mg/mL, LipCsP-Chitosan reduced the viability of Klebsiella pneumoniae by 57.45% ± 3.76 after 24 h. The results obtained from the current study offer a new approach to the utilization of LipCsP-Chitosan as nanocarriers for candidate anti-pneumococcal agents.
Development and Characterization of Nanovesicles Containing Phenolic Compounds of Carissa spinarum: Encapsulation, Release Kinetics, Antimicrobial Activity and Mathematical Modeling
(Trans Tech Publications Ltd, 2023-05) Rubaka, Clarence; Gathirwa, Jeremiah; Malebo, Hamisi; Swai, Hulda; Hilonga, Askwar
The aim of this study was to develop and characterize a delivery system for polyphenols from an extract of Carissa spinarum leaves, based on liposomes. Liposomes loaded with Carissa spinarum polyphenols (nanoliposomal CsP) were prepared by ethanol-solvent injection method and characterized in terms of zeta potential, size, and polydipersity index by using Zeta sizer and Fourier Transform Infrared spectrum analysis. Total Phenolic content was measured by using Folin-Ciocalteu method and entrapment efficiency was evaluated. The release behavior was conducted in Phosphate Buffer Saline (PBS) solution at pH, 7.4 and Kinetic model fitted to evaluate mechanism of release. Disc diffusion sensitivity test was used to evaluate antimicrobial activity of free extract and nanoliposomal CsP. The mean diameter of nanoliposomal CsP was 181 ± 1.02 nm and had 0.345 ± 0.014 polydipersity index. Zeta potential value for nanoliposomal CsP was-45.6 ± 8.84 mV. Entrapment efficiency under the optimum conditions was 66.11 ± 1.11%. and the nanoliposomal CsP was stable over 30 days. The antibacterial activity of nanoliposomal CsP exhibited inhibition zone diameter of 14.33 ± 1.53 mm and 12.00 ± 1.23 mm against S. aureus and E. coli respectively The results reveal the Carrisa spinarum liposome can be applied as potential carrier for delivery of polyphenols to improves therapeutic action against bacterial strain.
Development, characterization and antimalarial efficacy of dihydroartemisinin loaded solid lipid nanoparticles.
(Elsevier, 2016-04-01) Omwoyo, Wesley; Melariri, Paula; Gathirwa, Jeremiah; Oloo, Florence; Mahanga, Geoffrey; Kalombo, Lonji; Ogutu, Bernhards; Swai, Hulda
Effective use of dihydroartemisinin (DHA) is limited by poor water-solubility, poor pharmacokinetic profile and unsatisfactory clinical outcome especially in monotherapy. To reduce such limitations, we reformulated DHA into solid lipid nanoparticles (SLNs) as a nanomedicine drug delivery system. DHA-SLNs were characterized for physical parameters and evaluated for in vitro and in vivo antimalarial efficacy. DHA-SLNs showed desirable particle characteristics including particle size (240.7 nm), particle surface charge (+ 17.0 mV), drug loadings (13.9 wt %), encapsulation efficacy (62.3%), polydispersity index (0.16) and a spherical appearance. Storage stability up to 90 days and sustained release of drug over 20 h was achieved. Enhanced in vitro (IC50 0.25 ng/ml) and in vivo (97.24% chemosuppression at 2 mg/kg/day) antimalarial activity was observed. Enhancement in efficacy was 24% when compared to free DHA. These encouraging results show potential of using the described formulation for DHA drug delivery for clinical application.
Formulation, Optimization, and Evaluation of Moringa oleifera Leaf Polyphenol-Loaded Phytosome Delivery System against Breast Cancer Cell Lines
(MDPI, 2022-07-11) Wanjiru, Jecinta; Gathirwa, Jeremiah; Sauli, Elingarami; Swai, Hulda
Moringa oleifera leaf polyphenols (Mopp) were encapsulated with phytosomes to enhance their efficacy on 4T1 cancer cell lines. The Mopp were extracted via microwave-assisted extraction. Moringa oleifera polyphenol-loaded phytosomes (MoP) were prepared with the nanoprecipitation method and characterized using the dynamic light scattering and dialysis membrane techniques. The in vitro cytotoxic and antiproliferative activity were investigated with the (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazole) MTT assay. Acute toxicity was assessed using Swiss albino mice. An MoP particle size of 296 ± 0.29 nm, −40.1 ± 1.19 mV zeta potential, and polydispersity index of 0.106 ± 0.002 were obtained. The total phenolic content was 50.81 ± 0.02 mg GAE/g, while encapsulation efficiency was 90.32 ± 0.11%. The drug release profiles demonstrated biphasic and prolonged subsequent sustained release. In vitro assays indicated MoP had a low cytotoxicity effect of 98.84 ± 0.53 μg/mL, doxorubicin was 68.35 ± 3.508, and Mopp was 212.9 ± 1.30 μg/mL. Moreover, MoP exhibited the highest antiproliferative effect on 4T1 cancer cells with an inhibitory concentration of 7.73 ± 2.87 μg/mL and selectivity index > 3. The results indicated a significant difference (p ≤ 0.001) in MoP when compared to Mopp and doxorubicin. The in vivo investigation showed the safety of MoP at a dose below 2000 mg/kg. The present findings suggest that MoP may serve as an effective and promising formulation for breast cancer drug delivery and therapy.
In vitro antiproliferative potential of Annona senegalensis Pers. and Allophylus africanus P Beauv. plant extracts against selected cancer cell lines
(Journal of Medicinal Plants Research, 2019-07-10) Biseko, Emiliana Zacharia; Swai, Hulda; Mbugua, Regina Wachuka; Ndung’u, Jecinta Wanjiru; Chepng’etich, Jean; Gathirwa, Jeremiah
The medicinal plants Annona senegalensis Pers. and Allophylus africanus P Beauv. are used in Tanzania traditional medicine for the treatment of cancer. However, there is no scientific documentation on their therapeutic effectiveness. The present study evaluated antiproliferative potential as an indicator of anticancer activity of A. senegalensis and A. africanus plant species from Tanzania. A. senegalensis and A. africanus were collected from Ugweno village at Kilimanjaro, Tanzania. Different types of extracts were prepared in dichloromethane/methanol (DCM:MeOH), petroleum ether, DCM, ethyl acetate (EtOAc), MeOH and water respectively. Antiproliferative activity against HCC 1396 (breast), HEp-2 (throat) and CT 26 (colon) cancer cell lines was assessed by the MTT cell viability assay. The results of the present study showed that the antiproliferative activity varied between plant extracts and the cancer cell lines. The highest antiproliferative activity was achieved with petroleum ether extract of A. senegalensis against HEp-2 with an IC50 value of 0.42 ± 0.09 μg/ml. This also depicted the highest selectivity to cancerous cells (SI value 94.19) compared to the other extracts. A. africanus also depicted good antiproliferative activity against HEp-2 with IC50 values of 1.00 ± 0.41 and 2.37 ± 1.45 μg/ml for DCM:MeOH and petroleum ether extracts, respectively. The findings validate the traditional use of A. senegalensis and A. africanus in the treatment of cancer. Results also support previous studies which demonstrated the effect of extraction solvent used in extraction of bioactive agents from medicinal plants. Further studies involving the isolation of pure antiproliferative compounds against cancer cells from the two plants are recommended to elucidate bioactive molecules.
In vitro antiproliferative potential of crude extracts from Carica papaya L. (Caricaceae) black seeds against prostate cancer cell lines'
(American Journals, 2022-04-30) Kateihwa, Benson; Swai, Hulda; Gathirwa, Jeremiah; Sauli, Elingarami
Black seeds from papaya plants are utilized as traditional medicine in African and Asian cultures to improve the functioning of the male reproductive system and management of prostate cancer. This study analyzed the phytochemical composition, antiproliferative activity and cytotoxicity of Carica papaya black seeds against the prostate cancer cells and Vero cells. Phytochemical screening was performed by standard procedures. Methyl tetrazolium bromide (MTT) cell viability assay was used to evaluate the antiproliferative effect of crude extracts in prostate cancer cells against the control. Phytocompounds, namely flavonoids, alkaloids, tannins, terpenoids, glycosides and saponins were found in the crude extracts. All papaya seeds’ extracts had antiproliferative activity towards prostate cancer cells. Ethyl acetate extract was found with higher antiproliferative activity with IC50 of 3.64 µg/ml. The crude extracts were not toxic towards Vero cells as compared to the control. Isolation and characterization of active compounds from herein crude extracts and papaya black seeds are therefore recommended for future studies.
Inorganic Nanocarriers: Surface Functionalization, Delivery Utility for Natural Therapeutics - A Review
(Scientific.Net, 2022-08) Rubaka, Clarence; Gathirwa, Jeremiah; Malebo, Hamisi; Swai, Hulda; Hilonga, Askwar
Inorganic nanocarriers for a decade have increased interest in nanotechnology research platform as versatile drug delivery materials. The utility of the inorganic nanocarriers for delivery of therapeutic agents is attributed to their unique properties such as magnetic, photocatalytic nature and the ability to exhibit surface functionalization. Herein, we review the surface functionalization and delivery utility for natural therapeutics exhibited by inorganic nanocarriers mostly focusing on their magnetic, photocatalytic and the plasmonic properties. The review also highlights the influence of electronic property of inorganic surface on functionalization of ligand based natural therapeutic agents. Improvement of stability and therapeutic potential by formation of nanocomposites are detailed. Furthermore, we suggest improvement strategies for stability and toxicity reduction of inorganic nanoparticles that would potentially make them useful for clinical application as therapeutic delivery tools for treatment of various diseases.
Preparation, characterization, and optimization of primaquine-loaded solid lipid nanoparticles
(Dovepress, 2014-08-11) Omwoyo, Wesley; Ogutu, Bernhards; Oloo, Florence; Swai, Hulda; Kalombo, Lonji; Melariri, Paula; Mahanga, Geoffrey; Gathirwa, Jeremiah
Primaquine (PQ) is one of the most widely used antimalarial drugs and is the only available drug that combats the relapsing form of malaria. PQ use in higher doses is limited by severe tissue toxicity including hematological- and gastrointestinal-related side effects. Nanoformulation of drugs in an appropriate drug carrier system has been extensively studied and shown to have the potential to improve bioavailability, thereby enhancing activity, reducing dose frequency, and subsequently reducing toxicity. The aim of this work was to design, synthesize, and characterize PQ-loaded solid lipid nanoparticles (SLNs) (PQ-SLNs) as a potential drug-delivery system. SLNs were prepared by a modified solvent emulsification evaporation method based on a water-in-oil-in-water (w/o/w) double emulsion. The mean particle size, zeta potential, drug loading, and encapsulation efficiency of the PQ-SLNs were 236 nm, +23 mV, 14%, and 75%, respectively. The zeta potential of the SLNs changed dramatically, from −6.54 mV to +23.0 mV, by binding positively charged chitosan as surface modifier. A spherical morphology of PQ-SLNs was seen by scanning electron microscope. In vitro, release profile depicted a steady drug release over 72 hours. Differential scanning calorimeter thermograms demonstrated presence of drug in drug-loaded nanoparticles along with disappearance of decomposition exotherms, suggesting increased physical stability of drug in prepared formulations. Negligible changes in characteristic peaks of drug in Fourier transform infrared spectra indicated absence of any interaction among the various components entrapped in the nanoparticle formulation. The nanoformulated PQ was 20% more effective as compared with conventional oral dose when tested in Plasmodium berghei-infected Swiss albino mice. This study demonstrated an efficient method of forming a nanomedicine delivery system for antimalarial drugs.