International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (3), pp. 001-008, March, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
Regulation of Connexin Expression by Angiotensin Modulators (Losartan and Ramipril) in Vascular Injury
Xujuan Li, Deqiang Li, Jinfeng Duan, Junzhu Chen, Wei Cai* and Voonthow Kok
The First Affiliated Hospital, College of Medicine, Zhejiang University, No.79, Qingchun Road, Hangzhou, Zhejiang Province, P. R. China, 310003.
Accepted 27 July, 2024
Intercellular gap junction (GJ) plays a pivotal role in the proliferation and transformation of vascular smooth muscle cells (VSMCs). This study was designed to test the hypothesis that expressions of the component proteins of gap junctions, connexins40 and 43 (Cx40 and Cx43), are up-regulated in arteries subjected to balloon injury and that this up-regulation can be suppressed by statin therapy. Transmission electron microscopy (TEM) revealed that there were abundant GJ between neointimal SMCs but fewer and smaller GJ after losartan and ramipril treatment. Reverse transcription–polymerase chain reaction and Western blot analysis showed the messenger ribonucleic acid (mRNA) and protein expressions of Cx40 and Cx43 were elevated after injury, and these elevations were suppressed by losartan and ramipril. Immunostaining showed the Cx40 and Cx43 expressions were consistently enhanced in the neointimal area after injury, which was decreased by losartan and ramipril treatment. Balloon injury causes up -regulation of Cx40 and Cx43 in neointimal SMCs. angiotensin -converting enzyme inhibitors (ACEIs) and AT1 antagonist losartan can reduce the proliferation of SMCs, suggesting the rennin-angiotensin system (RAS) system plays an important role in the remodeling of GJ in the VSMCs under pathological conditions.
Key words: Vascular smooth muscle cell, gap junction, connexin, balloon angioplasty, statin.
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (3), pp. 001-005, March, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
The Influence of Chloroquine on Chlorpropamide Pharmacokinetics in Healthy Volunteers
Danlami U.1*, Odunola M. T.2, Magaji G.2 and Thomas S. A.1
1Sheda Science and Technology Complex (SHESTCO), P.M.B. 186, Garki, Abuja, Nigeria. 2Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria, Nigeria.
Accepted 07 October, 2024
The effect of chloroquine on the pharmacokinetics of chlorpropamide was investigated in human volunteers. The study was carried out by administering chlorpropamide alone on healthy volunteers, and then chlorpropamide was co-administered with chloroquine. High performance liquid chromatography (HPLC) was used for the analysis of the plasma levels of chlorpropamide. The solvent used was acetonitrile/water (6:4) at pH 6.7. Ultrasphere ODS column, 4.6 × 25 cm, USA was used. The result from the chlorpropamide plasma level analysis shows that the absorption half-life (t1/2a) and the time to maximum peak concentration (tmax) increased by 10% (P < 0.04) and 20% (P < 0.01), respectively. The absorption rate constant (Ka) and the maximum concentration (Cmax) decreased by 30 and 16% (P < 0.02), respectively. The area under the curve (AUC0-168) decreased significantly by 50% (P < 0.03). The plasma clearance of chlorpropamide increased significantly by 86% (P < 0.01).The volume of distribution (Vd) and the elimination half life(t1/2el) decreased by 10%(p<0.03) and 47% (P < 0.01), respectively, while the elimination constant (kel) increased by 100% (P < 0.02). Co-administration of chlorpropamide with chloroquine significantly (P < 0.05) impaired the absorption and elimination of chlorpropamide.
Key words: Pharmacokinetics, chlorpropamide, chloroquine, high performance liquid chromatography, half-life, absorption rate constant, elimination constant.
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (3), pp. 001-008, March, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
Transdermal Delivery of Ligustrazine Phosphate Using Microemulsions: A Formulation Investigation
Ying Cui1,2, Lingzhi Li1,2, Jun Gu1, Ting Zhang3* and Li Zhang1
1Department of Medicine Chemistry, Logistics University of Chinese People’s Armed Police Forces, Tianjin 300162,
P. R. China.
2Tianjin Key Laboratory of Occupational and Environmental Hazards Biomarkers, Tianjin 300162, P. R. China.
3Department of Pharmacy, Xiangya Hospital, Central South University, Changsha 410008, P. R. China.
Accepted 10 January, 2025
Ligustrazine phosphate is commonly used as an efficient drug to treat a variety of cardiovascular disorders with frequent administration for a short biological half-life. The purpose of the present study was to investigate a microemulsion system for transdermal delivery of ligustrazine phosphate for the convenient, efficient and safe administration. The existence regions of microemulsions containing isopropyl myristate, labrasol, plurol oleique® and water were investigated in pseudo-ternary phase diagrams, according to which microemulsion vehicles were prepared to observe average diameter, pH value, stability and evaluate respective effect of each component on percutaneous delivery in vitro. The prepared microemulsions had average diameters ranging from 32.1 to 108.7 nm, mild pH values and suitable stability. The optimized microemulsion with permeation flux of 41.01 g/cm2/h across rat skin in vitro, showed no obvious irritation on back skin of rabbits. The results indicated that the studied microemulsion system might be a promising vehicle for transdermal delivery of ligustrazine phosphate.
Key words: Microemulsion, transdermal delivery, ligustrazine phosphate.
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (3), pp. 001-007, March, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
Bioavailability Study of Four Aspirin Brands Marketed in Nigeria: An In Vitro-In Vivo Correlation Analysis
Bamigbola E. A.1*, Ibrahim M. A.2, Attama A. A.3 and Uzondu A. L.1
1Department of Pharmaceutics and Pharmaceutical Microbiology, Faculty of Pharmacy, Madonna University,
Elele, Rivers State, Nigeria.
2Department of Pharmaceutics and Pharmaceutical Technology, University of Jos, Plateau State, Nigeria.
3Department of Pharmaceutics, University of Nigeria, Nsukka 410001, Enugu State, Nigeria.
Accepted 30 January, 2025
The study investigated the possibility of developing an in vitro – in vivo correlation for four commercial brands of aspirin tablets using USPXXI rotating basket apparatus and urinary excretion profiles from eight human volunteers. Various dissolution and pharmacokinetic parameters were obtained for all the brands. Significant rank order correlations were observed between all the in vitro dissolution parameters such as percent dissolved at 30 min, dissolution rate constants (k) and time for 50% dissolution (DT50%) and all the in vivo bioavailability parameters such as cumulative amount excreted up to 8 h (E8), maximum excretion rate (dE/dt)max and time for maximum excretion rate (Tmax). However, no correlation could be established between the cumulative amount excreted up to 24 h (E24) and any of the in vitro dissolution parameters. Moreover, statistical analysis showed no significant inter-subject variation among the subjects that participated in the experiments.
Key words: Aspirin tablets, dissolution rate constant, maximum excretion rate, cumulative amount excreted, in vitro-in vivo correlation (IV-IVC).
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (3), pp. 001-010, March, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Review
Exploring the Phytochemical Profile and Therapeutic Potential of Kaempferia galanga L.
Muhammad Ihtisham Umar1*, Mohammad Zaini Bin Asmawi1, Amirin Sadikun2, Rabia Altaf1 and Muhammad Adnan Iqbal3
1Department of Pharmacology, School of Pharmaceutical Sciences, University Sains Malaysia,
11800 Pulau Pinang Malaysia.
2Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, University Sains Malaysia, 11800 Pulau
Pinang Malaysia.
3School of Chemical Sciences, University Sains Malaysia, 11800 Pulau, Pinang Malaysia.
Accepted 25 January, 2025
Kaempferia galanga L. (KG), commonly known as cekor is one of those precious medicinal herbs of Zingiberaceas that are still included in un-utilized herbs inspite of the variety of useful pharmacological properties it possesses. Extracts of KG have anti-inflammatory, analgesic, nematicidal, mosquito repellent, larvicidal, vasorelaxant, sedative, antineoplastic, antimicrobial, anti-oxidant, antiallergic and wound healing properties. Here, we have reviewed all the reported pharmacological properties of this valuable herb with an intention to highlight the effectiveness and potentials of this herb. Ethyl-p-methoxycinnamate and ethyl-cinnamate are found to be the most vital constituents responsible for most of these pharmacological properties. Antinociceptive effect of KG extracts is comparable with that of aspirin whereas its nematicidal effect is even more potent than Carbofuran and metham sodium.
Key words: Antinociceptive, nematicidal, cekor.
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (3), pp. 001-008, March, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
The Effects of Baicalin on Lipopolysaccharide-Induced Uterine Endometrium Damage and Implantation Failure in a Murine Model
Yantao Zhao1, Yongzhan Bao1, Wanyu Shi1,2, Xiaodan Wang2 and Xiuhui Zhong1,2*
1College of Veterinary Medicine, Agricultural University of Hebei, Baoding 071001, China.
2Institute of Traditional Chinese Veterinary Medicine, Agricultural University of Hebei, China.
Accepted 4 January, 2025
The objective of this study is to investigate the protective effects of baicalin and to elucidate its immunological modulation at maternal-fetal interface. Lipopolysaccharide (LPS) was given via intraperitoneal injection to induce embryo implantation failure in mice which received baicalin at days 0.5 to 3.5 of gestation. The IFN- /IL-10, nitric oxide synthase (NOS) activities of uterine and endometrial tissues in each group (n = 16) were detected by ELISA, respectively. The ratio of IFN- /IL- 10 and NOS activities increased significantly in the uterus of LPS-induced mice implantation failure and endometrial cells of LPS interference. In the baicalin pretreated mice followed by LPS administration, the ratio of IFN- /IL-10 and NOS activities were normalized by the middle dose baicalin to the control level, significantly lower than LPS treatment group. The same results were received in vitro study of LPS interference endometrial cells. The results indicate that baicalin has protective effects through inhibiting excessive IFN- and NO production to modulate the immunological balance at maternal-fetal interface.
Key words: Baicalin, lipopolysaccharide (LPS), implantation failure, IFN- , IL-10, nitric oxide (NO).
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (3), pp. 001-005, March, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
Evaluating the Antiplasmodial Activity of Sphenocentrum jollyanum Pierre Leaf and Root Extracts In Vivo
O. S. Olorunnisola* and A. J. Afolayan
School of Biological Sciences, University of Fort Hare, Alice 5700, South Africa.
Accepted 16 January, 2025
Methanolic leaf and root extracts of Sphenocentrum jollyanum Pierre were tested in vivo for anti-malarial activity in Swiss albino mice inoculated with chloroquine resistant Plasmodium berghei NK 67 strain. The two extracts exhibited a significant (p>0.05) dose dependant anti- plasmodial activities in isolation and when combined in the 4-days curative standard test with a high mean of survival time. Although, the standard drug, Arthemether - lumefartrin, showed the highest antimalaria potency (81.4%), those of the leaf (74.4%) and root extracts (54.1%) in isolation and combination (63.4%) compared favorably. The leaf extract demonstrated higher antimalarial potency than the root or combination. The two extracts also produced a significant (p>0.05) positive effect on the weight and hematology values in the treated animals. Phytochemical screening of the plant (leaf and the root extracts) reveals the presences of flavonoids, steroids, terpenoids, tannins and alkaloids. The anti-plasmodia activity of these plant extract might be attributed to these phytochemicals compounds. The results showed that the leaf and root of S. jollyanum possesses an anti-malarial activity which was effective against chloroquine resistance strain. This work has validated the traditional uses of S. jollyanum root extract in the treatment of malaria and also reported for the first time the anti-malarial property of the S. jollyanun leaf extract.
Key words: Sphenocentrum jollyanum, Plasmodium berghei, Arthemther lumefartrin, hematological parameter, anti-plasmodium.
