Journal of Drug Delivery and Therapeutics (JDDT)
Not a member yet
4948 research outputs found
Sort by
Novel Applications of Hot Melt Extrusion Technology
Get PDFHot melt extrusion (HME) technology was introduced to pharmaceuticals in the 1970s for manufacturing and product development. Since then, there were several developments in HME technology to utilize it effectively for the manufacturing of pharmaceuticals. Though the primary purpose of HME technology remains to be solubility enhancement through the preparation of amorphous solid dispersions, it also has various other applications like dry granulation, abuse-deterrent formulation, continuous manufacturing, film preparation, implants, sustained release formulations, etc. The purpose of this review article is to consolidate the information related to applications of HME technology in the pharmaceutical industry.
Keywords: Hot melt extrusion, poorly soluble drugs, continuous manufacturing, solid orals, and applications
Evaluation of acute, subacute toxicity and in vivo impact of aqueous decoction of Flemingia faginea Guill. & Perr. (Barker) leafy stems on NMRI mice and normotensive Wistar rats
Get PDFIntroduction: Flemingia faginea, a Fabaceae family medicinal plant, has been used for a long time in Burkina Faso for the treatment of hypertension and excess salt. However, the safety of the preparations derived from this plant has not yet been scientifically documented. This study aimed to evaluate the acute and subacute oral toxicity of the leafy stems aqueous decoction of F. faginea (FAD) in healthy normotensive mice and rats and the impact on their normal blood pressure. Material and Methods: The acute oral toxicity study was conducted according to the toxicity class method of the Economic Cooperation and Development Organization (OECD) guideline 423. Subacute toxicity was carried out according to the OECD Guideline 407 for repeated dose chemical toxicity for 28 days. Hematological and biochemical analyzes of blood were performed after autopsy. An evaluation of the impact of the extract on the blood pressure of rats was performed using the non-invasive method. Results: A single oral dose of 2000 mg/kg bw to mice did not cause mortality or clinical signs or symptoms of toxicity during the 14-day study. The FAD was classified in the fifth category of the Harmonized System of Classification of the United Nations and considered practically safe with an estimated 50% lethal dose of 5000 mg/kg bw. Daily gavage of male and female rats with doses of 100,500 and 1000 mg/kg did not result in mortality or significant adverse effects during the 28days of experimentation. There were no significant differences in body weight gain, food &water consumption or relative vital organ weights in treated animals. Analysis of the hematological and biochemical parameters of blood serum did not show significant differences between treated and control animals in this study. Additionally, no aberrant changes were found in the systolic and diastolic blood pressures of the test animals during the 28 days of inclusion compared to those of the control group. Conclusion: The extract FAD could be considered safe within the doses tested for the results of the toxicological evaluation. However, microscopic, histopathological, and subchronic investigations will have to be carried out to confirm the safety of this extract use
Acemetacin in Acute and Chronic Pain Management
Get PDFAcemetacin is the carboxymethyl ester of indomethacin and is a pro-drug precursor compound, in other words, a prodrug. The pharmacologically active metabolite of acemetacin is also indomethacin. Acemetacin exerts its potent non-steroidal anti-inflammatory effects in the body as indomethacin. It is known that acemetacin is not only a prodrug of indomethacin, but also an agent with gastric protective mechanisms, possibly involving a reduction in leukocyte adhesion, and that acemetacin exerts gastric protective effects by exhibiting less efficacy on the COX-1 enzyme in the gastric mucosa compared to direct indomethacin use. It is clear that acemetacin is a valuable NSAID for acute and chronic pain.
Keywords: Acemetacin, indomethacin, non-steroidal anti-inflammatory drugs
Drug-Induced Liver Injury from Anti-Tuberculosis Treatment in a Case of TB Meningitis
Get PDFThis case study revolves around a 38-year-old male patient who arrived at the Emergency department complaining of decreased levels of consciousness, agitation, and disorientation. The case follows his admittance to the ICU, while a team of doctors worked on finding a possible diagnosis for his condition.
It was later in the course of his disease that it was found from his CSF(Cerebrospinal fluid) sample that he was suffering from tuberculous meningitis. The culture result revealed a strain of Mycobacterium Tuberculosis that was sensitive to all the major anti-tuberculous drugs. This was a favorable point for the prognosis of this patient. Once he was started on a regimen of selected anti-TB drugs, his symptoms improved to the point of successful discharge from the hospital.
However, a few days later, the patient again started experiencing symptoms that were serious enough to justify hospital admission. It was found that it was not any primary issue causing the symptoms this time, but rather the toxicity of the anti-tuberculous drugs. However, due to timely diagnosis, intervention, and management, his condition was managed effectively and he was discharged once again.
This case study aims to measure the importance of prescribing the most effective yet adequate treatment regimen for all patients, keeping in mind several overlooked yet highly important health-related factors that could either exacerbate or deteriorate pre-existing health concerns in a given patient. If the patient had been evaluated carefully for any underlying liver diseases or been given a short trial to see if he could withstand the high dose of anti-tuberculous drugs, he would not have faced such dreadful consequences, though they were managed quickly.
Keywords: Cerebrospinal fluid, Mycobacterium Tuberculosis, liver diseases, anti-tuberculous drugs
Molecular Characterisation of Multidrug Resistant Pathogen Isolated from Egg and its Control Measures
Get PDFMultidrug resistance is a condition enabling a disease causing microorganism to resist distinct drugs or chemical of wide variety of structure and function targeted at eradicating the bacteria. Microorganisms that display multidrug resistant can be pathogenic cells. In this study, table eggs are used commonly, because it considered the most nutritious economical source of protein that can be a part of healthy diet. However, egg shell carries bacteria which cause illness; even unbroken clean fresh shell egg may also contain harmful bacteria. In egg shell presence of Escherichia coli and Staphylococcus aureus were found. Out of total examined sample, no Salmonella was detected. Several disease occurred in poultry are caused by Staphylococcus sp. such as Staphylococcus aureus. It produces Enterotoxins which create food poisoning in consumers. Eggs are the potential source of transmitting antibiotics. Resistant Staphylococcus strain to human causing food-borne infection through Staphylococcus strains can potentially be harmful to humans. Methicillin-resistant Staphylococcus aureus (MRSA) is considered as one of the important bacterium. As a result, Multidrug resistance (MDR) in the bacteria may develop. Nowadays poultry farm increase day by day in Tamilnadu, there is a chance of transmitting the MRSA to Human through egg consumption. This present study was conducted to isolate the bacterial species and the characterization of Staphylococcus aureus along with remedial measure on egg Shell surface.
Keywords: Multidrug resistant, Pathogenic, Egg shell, Antibiotics, Human welfar
Formulation and Evaluation of New Sustained Release Floating Microspheres of Cilnidipine by Solvent-Diffusion Evaporation Technique
Get PDFThe purpose of the present investigation was to develop a gastro-retentive cilnidipine loaded floating microspheres. The floating microspheres of cilnidipine were prepared by the solvent evaporation method for oral drug delivery using HPMCK4M and ethyl cellulose as polymers. The drug loaded microspheres were evaluated for particle size, drug content, entrapment efficiency and floating time. The in-vitro study was performed in pH 1.2 to determine the amount of drug released. Field emission scanning electron microscopy (SEM) was performed to check the surface morphology of microspheres. The mean particle size of the microspheres was in the range of 226.85 – 339.42µm. The drug content of the floating microspheres was more than 70% and drug entrapment efficiency of microspheres obtained between 64.64 – 83.0%. The in-vitro buoyancy was more than70%. Cumulative % of drug release obtained between 73.12 – 89.68%. Field emission scanning microscopy results showed that the prepared microspheres were smooth and spherical.The study reveals that more the particle size extended the floating time, this methods reveals that the drug content of the microspheres enhanced as the amount of polymer increased or increased in ethyl cellulose concentration also leads to increase in entrapment efficiency and particle size. Cumulative % drug release decreased as ethyl cellulose concentration increased.
Keywords: cilnidipine, microspheres, floating drug delivery system, entrapment efficiency, cumulative drug release, ethyl cellulose, Field emission scanning electron microscopy, polymer, concentratio
Application of Artificial Intelligence and Machine Learning in Drug Discovery and Development
Get PDFDrug discovery has traditionally been a time consuming and expensive endeavor. Additionally, drugs weren’t as effectively designed as those that are being predicted and developed through AI and ML today. Machine learning is a form of artificial intelligence that develops and evolves based on experience (similarly to the human mind), and is more recently being utilized in drug discovery and design. The integration of AI and ML into the drug discovery and development process has allowed for higher target precision, lower toxicity, and better dosage formulations. AI more generally has been introduced to and has been leveraged at, each step of drug development, including target identification and validation, hit identification, as well as hit to lead optimization, and has been key in shortening the previously lengthy drug screening process. AI and ML has also been applied downstream in drug formulation where it has maximized resource utilization and is allowing for web-based 3D printing of drugs. Application of AI in the drug development process has also been extended to the modeling of novel drug-like compounds to predict their ADMET properties. This review will address the stages of drug discovery and development in which the application of AI and ML modeling has altered the traditional development of drugs.
Keywords: Drug discovery, machine learning, artificial intelligence, computational drug development
Formulation and Evaluation of Nanoemulgels for the Topical Drug Delivery of Posaconazole
Get PDFObjective: Posaconazole(POS) is an antifungal drug widely used in treatment of fungal infections. However, the drug has very low oral bioavailability due to high first-pass metabolism, thereby limiting its therapeutic effectiveness. The present study is aimed to prepare nanoemulsion of posaconazole to increase its solubility and to develop posaconazole-loaded nanoemulsion based gel for single dose topical administration to sustain the release of the drug, improve patient compliance and avoid repeated administration.
Method:-FTIR-study was performed to determine compatibility of drug with excipients. Pseudoternary-phase diagram was constructed to optimize the Smix ratio. Optimization of nanoemulsion was done by Box-Behnken Design. The optimized formulation was evaluated for particle-size (nm), polydispersity index (PDI), (%) drug content and in-vitro drug release. POS-nanoemulgel (FNG) was developed using carbopol-934P (1%), which was evaluated for homogeneity, pH, viscosity, spreadability, percentage-yield and in-vitro drug release. The anti-fungal activity of POS-nanoemulgel was evaluated against Candida Albicans.
Results: The FTIR-study confirmed that there was no interaction between drug and excipients. The optimized selected nanoemulsion (FN1) exhibited particle size 79.19nm, PDI 0.357, drug content 95.90% and in-vitro release of 79.40% at 24 hour. The prepared nanoemulgel was homogenous, opaque with good spreadability 13.91±1.19, viscosity 3760±0.014, pH 5.6±0.06 and the zeta-potential was -29mV, indicating good stability. The drug release at 24h was 72.01%. Further, the developed nanoemulgel formulation exhibited better antifungal activity in comparison to the pure drug gel.
Conclusion: Hence, it can be concluded that nanoemulgel of posaconazole can provide better antifungal activity and improve patient compliance.
Keywords: Nanoemulsion, Nanoemulgel, Posaconazole, Anti-fungal, Box-Behnken Design, Pseudoternary phase diagram
Molecular Docking Analysis of Piperonal and its Analogues as Promising Cancer Therapeutics by Modulating Angiogenesis
Get PDFCancer is an emerging disease that pose severe public health problem that has a poor prognosis at early stage encompassing small number of effective therapies leading to high mortality rate at an alarming rate. The cancer cell multiplication and growth can be arrested at an early metastasis stage by inhibiting VEGF involved in angiogenesis. Hence in the present study, insilico approach is followed to screen piperonal and its significant analogues for inhibitory role against VEGF. The molecular properties were analysed using Molinspiration and molecular docking analysis was performed using Glide Schrodinnger. The compounds tenamfetamine and midomafetamine showed better binding strength when compared with Sorafenib.
Keywords: Piperonal, Structural Analogues, Angiogenesis, Metastasis, VEGF, Molecular docking, Autodock
Fecal carriage of extended spectrum beta-lactamase and fluoroquinolone resistant gene in non-typhoidal Salmonella enterica isolates from food-producing animals and humans
Get PDFThis study seeks to determine the feacal carriage of extended spectrum beta-lactamase and fluoroquinolone resistant non-typhoidal Salmonella enterica isolates from food-producing animals and humans. A total of three hundred (300) fecal samples were collected using sterile universal containers from food-producing animals namely (Chicken [100], Pig [100] and humans (100) from Onicha Local Government Area of Ebonyi State and analyzed for the presence of non-typhoidal Salmonella enterica using standard microbiological techniques. Phenotypic detection of extended-spectrum beta-lactamase (ESBL) were done by disc diffusion and Double Disk Synergy Test. Molecular characterization for ESBL and fluoroquinolone-resistant genes were done by PCR with specific primers. The result shows that non-typhoidal Salmonella species (NTS) accounted for 25 % and 17 % in poultry and pig fecal sample respectively while 60 % and 40% were phenotypic ESBL producers respectively. When compared statistically there is significant difference among isolates confirmed ESBL-positive (P˂ 0.05). Also, none of the 16 (58 %) NTS isolated from humans harbored ESBL phenotype. PCR analysis with β-lactam specific primer detected the presence of blaOXA 50 % and 50 %, blaSHV 36 %, and 64 %, blaTEM 43 % and 57 %, blaCTX-M 36 % and 64 % in poultry and pig respectively. Fluoroquinolone resistant gene QnrA was present in 0 and 100 % of poultry and pig respectively. QnrB was 40 % and 60 % in poultry and pig isolates respectively. QnrS was present in 64 % isolates of poultry and 13 % isolates in pig. The high prevalence of genes encoding beta-lactamases and fluoroquinolone resistance (TEM, SHV, CTX-M and OXA, (qnrA, qnrB and qnrS) were present more in poultry and pig than in humans and demonstrate a significant public health threat from consumption of food-producing animal harboring such pathogenic resistant genotype if not properly controlled.
Keywords: Extended spectrum beta-lactamase, Fluoroquinolone, non-typhoidal Salmonella enterica, feacal carriag