Journal of Drug Delivery and Therapeutics (JDDT)
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Identification of Betulinic Acid and Trimethoxyellagic Acid as the Antidiabetic Compounds in Anogeissus leiocarpus Stem Bark Purified Extract
Get PDFObjectives: The study aimed to identify the antidiabetic compounds purified from stem bark of Anogeissus leiocarpus and propose the mechanisms of action.
Design: Anogeissus leiocarpus stem bark was purified through ethyl acetate and n-hexane with minor exceptions. For very clear separation, cold acetone was added to trigger the precipitation. The precipitate was dissolved with a mixture of DCM:methanol (9:1), adsorbed it to silica gel (5 g), evaporated to free flowing powder and fractionated it over silica gel (50 g) to realize 40 fractions. The gummy fractions were ignored. The light brown powder which possessed antidiabetic effect was selected for Nuclear Magnetic Resonance for structural elucidation.
Nuclear Magnetic Resonance (NMR) and Determination of Structure of Purified Compound: After column chromatography and TLC processes, along with the cold acetone, to the point of crystallization, the purified compounds, the light brown powder, were presented to NMR (Bruker Avance III, Spectrometer frequency 400 MHz; solvents DMSO-do, CDCl3, Acetone-d6. Institute of Chemistry, Strathclyde University Glasgow UK.) for determination of compound structures and analyses.
Results: The NMR spectra and analyses revealed the existence of Betulinic acid and Trimethoxyellagic acid.
Conclusion: We show that Betulinic acid and Trimethoxyellagic acid are potent antidiabetic compounds in the stem bark extract of A. leiocarpus.
Keywords: Anogeissus leiocarpus, Betulinic Acid, Trimethoxyellagic Acid, Antidiabetic agen
Androgenic effects of the aqueous extract of Pycnanthus angolensis (Welw.) Warb. (Myristicaceae) wood in hemicastrated male Wistar rats: Aqueous extract of Pycnanthus angolensis (Welw.) Warb alleviates the effects of castration
No full textBackground: Androgen deficiency is the most common disorder of reproductive function and can lead to male sexual disorders.
Objective: This study was designed to evaluate the androgenic effects of Pycnanthus angolensis (Welw.) Warb in hemicastrated rats.
Materials and methods: Forty-two male rats were divided into 6 groups of 7 rats each, including a group of uncastrated rats that received distilled water (10 ml/kg); a group of castrated rats that received 10 ml/kg of distilled water; a group of castrated rats that received testosterone enanthate (3 mg/kg BW) per week intramuscularly; and 3 groups of castrated rats that received 43, 86 and 172 mg/kg of the aqueous extract of Pycnanthus angolensis, respectively. After 14 days of oral treatment, the rats were killed by decapitation. The blood was collected and the androgen-dependent organs were collected for histological sectioning, and biochemical analysis. The tail of the epididymis was used to assess sperm quality.
Results: Treatment with the aqueous extract at doses of 43 and 86 mg/kg, significantly improved the sexual behavior of castrated rats, with increases of 25.92% and 22.74% intromissions frequency, and 67.06% and 56.46% mount frequency, compared to those in the castrated rats which did not receive any treatment. The extract also enhanced sperm quality in castrated rats. Both doses also significantly increased serum testosterone levels with rates of 45.07% and 49.00%, respectively; compared to those in the negative control group.
Conclusion: In view of the aforesaid results, Pycnanthus angolensis (Welw.) Warb could be considered as a promising natural agent in hypogonadism management.
Keywords: Androgen, hypogonadism, castrated male rats, unilateral castration, Pycnanthus angolensis (Welw.) War
Review on Nanogel as a Novel Platform for Smart Drug Delivery System
No full textOne of the most popular applications of nanotechnology in both topical and internal medicine administration to the body is nanogel technology. The materials comprising the nanoparticulate frameworks are less than 100 nm in a single measurement. The goal of this review paper is to provide a concise overview of the most recent developments in the nanogel medicine delivery framework with regard to drug loading and swelling. It categorises according to links (chemical and physical) and responding behaviour. This article is to give a broad overview of nanogels, their innovative use in many contexts, and current synthesis techniques. NGs use drugs for a variety of reasons, including diagnostics, gene targeting, organ targeting, and many more. Different pulmonary, nasal, transdermal, intra-ocular, oral, and parenteral routes can be used to give NGs. The primary goals of this review are to present broad details on NGs, their characteristics, multiple categories, medication targeting strategies, kinds of drug delivery systems, assessment techniques, and cutting-edge uses for NGs in depth.
Keywords: Nanogel, DLS, CD, mechanism of drug release, classification, applicatio
An Updated Overview of Gastro-retentive Floating Drug Delivery Systems: Formulation Strategies and Application
Get PDFGastro-retentive floating drug delivery systems (GRFDDS) have emerged as a significant advancement in enhancing the bioavailability and therapeutic efficacy of various medications. This review article provides a comprehensive overview of recent innovations in GRFDDS, highlighting their formulation strategies, mechanisms of buoyancy, and various applications in drug delivery. The role of various polymeric materials, gas-forming agents, and optimization techniques is discussed which are generally employed to develop effective floating systems. Additionally, keen insight is brought on applications of GRFDDS in treating gastrointestinal disorders, enhancing the pharmacokinetics of drugs with narrow absorption windows, and their potential in controlled-release formulations. In this review, authors compiled the recent reported literatures about the gastro-retentive floating drug delivery systems since 2015 to underline the effectiveness and safety profiles of these systems. This review aims to consolidate current knowledge and inspire future research directions in the development of GRFDDS for improved patient outcomes.
Keywords: Floating; Gastro-retentive; drug delivery; HPMC; Effervescen
Synthetic and Natural Polymers Enhancing Drug Delivery and Their Treatment: A Comprehensive Review
Get PDFPolymers, both synthetic and natural, play a critical role in modern drug delivery systems by enhancing the efficacy, targeting, and release profiles of therapeutic agents. This comprehensive review delves into the various types of synthetic polymers such as poly (lactic-co-glycolic acid) (PLGA), polyethylene glycol (PEG), and polyvinyl alcohol (PVA), as well as natural polymers like chitosan, alginate, and gelatin. These polymers are explored for their potential to improve solubility, bioavailability, and controlled release of drugs. Moreover, their application in targeted drug delivery, particularly for cancer, cardiovascular, and inflammatory diseases, is highlighted. The review also compares the advantages and limitations of synthetic versus natural polymers, discussing their biodegradability, biocompatibility, and regulatory considerations. Advances in polymer-based drug delivery platforms such as nanoparticles, hydrogels, and micelles are also examined, offering insights into future directions in personalized medicine. The highlights of provide in the review article, initially basics of drug delivery, polymer, polymerization with role of polymer in polymerization. At intermediate, classification, sources of polymer with that some advanced approached in drug delivery and lastly, marketed, recent available products with future challenges and current status in the drug delivery.
Keywords: Biodegradable polymer; natural; compatible; drug delivery; treatment; enhancing; polymers
In vitro Cyclooxygenase inhibitory activity and GC-MS profiling of bioactive compounds in Bauhinia racemosa Lam.
Get PDFNon-steroidal anti-inflammatory drugs (NSAIDs) are a common treatment for chronic pain and inflammation. While NSAIDs have been shown to reduce inflammation and pain associated with them, they have an array of side effects. Researchers investigated the COX inhibitory action of NSAIDs. They revealed that there are two distinct COX enzymes: COX-1 and COX2. Developing COX inhibitors has remained critical for producing innovative and safe anti-inflammatory drugs. Bauhinia racemosa Lam belonging to the family Fabaceae has a wide range of medicinal properties. The plant is used to treat various diseases in traditional medicine, but there is less knowledge based on clinical efficacy as an anti-inflammatory agent. In the present study Bauhinia racemosa Lam hydroalcoholic extract were screened for COX inhibition and GC-MS analysis was done to screen phytochemicals. The results obtained were found to inhibit 89% of COX activity significantly as compared to standard drug (Diclofenac sodium). GC-MS analysis revealed a total of ten potent bioactive compounds. The samples were identified by comparing retention time and peak area to literature and interpreting mass spectra. Results observed from the study suggest that the hydroalcoholic extract of Bauhinia racemosa Lam possess anti-inflammatory activity and can be utilized as an alternate source for NSAIDs.
Keywords: COX, Bauhinia racemosa Lam, Anti-inflammatory, NSAIDs
Evaluation of ethanolic extract of Piper methysticum leaves on anxiolytic activity of mice
Get PDFThe ethanol extract of Piper methysticum, commonly known as kava, has shown promising results in reducing anxiety. Studies suggest it may have anxiolytic effects, potentially offering a natural alternative to conventional anxiety treatments. The ethanolic extract of Piper methysticum can increase the duration of action. It can also increase the time spent in open arm, entry in open arm (in elevated plus model) as well as increase the time spent in light field (in Light Dark field) thus we can conclude that it can also possesses Anxiolytic action. The ethanolic extract of Piper methysticum possesses an anxiolytic like activity without sedative side effect. The corticosterone level in mice is increased when they got anxiety. So when the plasma corticosterone level of mice is checked in control group its turn out to be 10.28±0.52. It gets decreased with increase in doses. When treated with low dose of Aqueous extract is 7.28±1.44 is less effective than low dose of Ethanolic extract that is 6.22±1.28. Same as that high dose of extract shows the corticosterone level was 6.24±2.28 which was also less effective than high dose of ethanolic extract which was 5.52±0.32. Most effectively stress was decreased when treated with the Standard drug (Alprazolam) which shows plasma corticosterone level was 1.24±0.36. The mice of Piper methysticum extract (300 &600 mg/kg/ p.o.) treated group showed significantly (p<0.05) increased in body water intake as compared to the control group. Results showed that synthesized extract is very effective for the treatment of anxiety.
Keywords: Piper methysticum; anxiolytic activity; Anthraquinones; Light Dark mode
Inhibitory activity of nanoencapsulated quercetin against sodium arsenite-induced sub-acute liver toxicity in rats
Get PDFArsenic, a metalloid toxicant, is associated with a major global health problem as oxidative stress, a prime cause of tissue toxicity. The subject of our investigation was to assess the therapeutic efficiency of nanoencapsulated quercetin (QC) in combating sodium arsenite (NaAsO2)-inducted sub-acute hepatocellular toxicity in rat model. The rats of the hepatic damage group were injected subcutaneously (s.c.) four dosages of NaAsO2 (92.36 µM/kg b.wt.) twice a week. The rats of the polylactide nanoencapsulated QC group were injected intravenously (i.v.) four doses of nanoencapsulated QC (8.97 µmol/kg b.wt.) twice a week 2 h after the treatment (s.c.) with 92.36 µM /kg b. wt. NaAsO2 twice a week for four doses. The rats of the empty nanocasule or free QC treated group were injected i.v. four doses empty nanocapsule or free QC twice a week 2 h after the treatment (s.c.) with same doses of NaAsO2 twice a week for four doses. Arsenic deposition (580±20 µg/g protein) observed in liver tissue of rats treated with arsenite (92.36 µM/kg b.wt.), was found to reduce (120±9 µg/g protein) by the treatment of nanoencapsulated QC in rats significantly (p<0.001). The levels of antioxidant enzymes and GSSG/GSH ratio enhanced (p<0.001/0.1/0.01) by the treatment of NaAsO2 were reduced by the post treatment of nanoencapsulated QC significantly (p<0.001/0.01). The levels of ROS, lipohydroperoxide or membrane microviscosity increased or decreased (p<0.001) by the treatment of NaAsO2 were monitored to reduce or enhance significantly (p<0.001) by the treatment of nanoencapsulated QC in rat liver respectively. The blood serum biochemical levels enhanced (p<0.001) by the treatment of NaAsO2 were found to reduce significantly (p<0.001) by the treatment of nanoencapsulated QC in rats. The TGFβ1 and MMP-13 in the rat plasma augmented (p<0.001) by the treatment of NaAsO2-exposure were found to decline (p<0.001) significantly by the treatment of nanoencapsulated QC in rats. The rats in the other groups such as empty nanocapsule or free QC treated showed no or less inhibitory efficiency against NaAsO2-treatment compared to nanoencapsulated QC treated group. Application of nanoencapsulated QC may be a potent formulation to get higher inhibitory therapeutic efficiency against NaAsO2-induced sub-acute hepatocellular toxicity.
An Investigation of Antiepiletic Activity of Plant Extracts in Experimental Animals
Get PDFThe current study is done on plant extracts as antiepileptic medication in ayurvedic formulation. The convulsions are induced by electro shock therapy or picrotoxin, strychnine/brucine. After induction of convulsion the plant extract is administered as standard group, control group and simple group of six albino rats and the results are screened and analyzed with standard drug comparision. Pre-treatment of MEIR (methanolic extract of Ipomoea reniformis) for 15days at the dose of 200 and 400 milligram per kilogram body weight was used to evaluate antiepileptic activity. The antiepileptic activity was studied against seizures induced by Maximum electro shock (MES) in rats, Isoniazid (INH) and Pentylenetetrazol (PTZ) in mice.. In pre-treatment studies of antiepileptic activity, MEIR significantly (p<0.01) reduced the tonic hind limb extensor phase in MES model at 400milligram per kilogram body weight, while in INH, PTZ models at the dose of 200 and 400 milligram per kilogram body weight MEIR significantly (p<0.01) delayed the onset of clonic and tonic convulsions. The results of the Pr (+) study suggest that the MEIR possess antiepileptic activity in rats and mice. The results of each activites are compared with standard medicament and evaluated.
Keywords: Ipomoea reniformis, maximal electroshok, isoniazid, pentylenetetazol, convulsions, antiepileptic activit
Time to Cure and Predictive Factors Among Patients with Multi-Drug Resistance Tuberculosis in Puntland, Somalia: A Retrospective Cohort Study
Get PDFBackground: Multi-drug-resistant tuberculosis, also known as MDR-TB, is caused by bacteria that are resistant to the most effective first-line anti-tuberculosis medications, which are rifampicin and isoniazid. MDR-TB is an increasing global concern, and its spread has varying cure times for patients affected. Thus, this study was intended to investigate the median time to cure and identify predictive factors for patients with MDR-TB in Puntland, Somalia.
Methods: A retrospective cohort study was carried out at the MDR-TB center in Galkayo, Puntland, Somalia between the years of July 2017 and August 2023. The study utilized data that were collected from the inquiry form and monitoring cards of a randomly selected sample of 130 patients over a 6-year period. The data were entered into Epi-Data version 4.3 and analyzed using R Programming version 4.4.0. Non-parametric methods were used to estimate the median time to cure for patients with MDR-TB. Semi-parametric and parametric models were employed to determine predictive factors that influence the time to cure for MDR-TB patients. The Akaike Information Criteria (AIC) and Bayesian Information Criteria (BIC) of different survival models were compared to select the model that offers the best fit.
Results: Out of the total of MDR-TB patients, 109(83.85%) were cured and 21(16.15%) were censored during the follow-up period. The median time to cure from MDR-TB was found to be 619 days which is approximately 20 months. In accordance with the AIC and BIC, the Log-logistic accelerated failure time model was the best fit for the data as compared to the other AFT models. The result of the Log-logistic AFT model revealed that age, sex, disease site, and comorbidities significantly affect the time to cure for MDR-TB. According to this study, older age with MDR-TB patients, male MDR-TB patients, MDR-TB patients with comorbid conditions, and extrapulmonary MDR-TB patients had a longer time to cure than their reference categories.
Conclusion: Based on the findings of the study, the median time to cure for patients with MDR-TB in Puntland was found to be 20 months. Sex, disease site, comorbidities and age were predictive factors of time to cure from MDR-TB.