Journal of Drug Delivery and Therapeutics (JDDT)
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Khatmī (Althea officinalis L. and Althea rosea): Medicinal importance in the perspective of Unani medicine and pharmacological studies
Althea officinalis L. is an important Unani Medicinal plant belonging to the family Malvaceae. The herb is commonly known as Khatmī and Marsh-mallow. All parts of the plant such as seeds, leaves, root and flowers are mainly used as medicine in Unani Medicine. It is used for many pharmacological actions like diuretic, lithotriptic, deobstruent, anti-inflammatory, emmenagogue which makes it useful in treatment of kidney stone jaundice, menstrual disorder, hepatitis, headache etc. Many scientific studies are done on the pharmacological actions of this herb. In this chapter both modern and Unani perspective of pharmacological properties of Althea officinalis L. along with its Phytochemistry and pharmacological studies are included.
Keywords: Althea officinalis L.; Khatmī; Malvacea
In-Vitro Comparative Study of Levocetirizine Dihydrochloride and Montelukast Sodium Release Profiles in Xyzal M Suspension and Other Marketed Syrup Formulations
Objectives: In-vitro comparative analysis of the release profile of levocetirizine dihydrochloride and montelukast sodium in Xyzal M Suspension and three commercially available syrup formulations.
Method: The active components and their impurities were initially assayed in all formulations using a validated HPLC method. The enantiomeric impurities of montelukast sodium in different pH media were determined using the HPLC method specified in the United State Pharmacopoeia (USP) monograph. Additionally, dissolution studies and the soluble fractions of the components were evaluated in pH media that mimic the conditions of the gastrointestinal tract. The particle size was also analyzed using microscopic analysis. All parameters were examined in fresh, stressed, and aged samples of each formulation.
Results: The assay results indicate the claimed potency of formulations. The total and enantiomeric impurities meet the limits set by the Indian Pharmacopoeia (<2%) and USP monograph (<0.2%), respectively. The particle size analysis demonstrated that montelukast remained suspended throughout the Xyzal M suspension. Levocetirizine in all formulations exhibited a soluble fraction of >70% after 1 and 24 hours in various pH media. For montelukast, the soluble fraction exceeded 50% in all syrup formulations. However, in Xyzal M suspension, montelukast was found to be 100% insoluble in all pH media after 1 and 24 hours, except in simulated intestinal fluid (~40-45%) after 24 hours. The absence of S-enantiomer, even in simulated intestinal fluid, indicates its presence in the pharmacologically active form.
Conclusion: Xyzal M suspension is a promising dosage formulation for achieving desired pharmacological action, outperforming the syrup formulations.
Keywords: Levocetirizine dihydrochloride, Montelukast sodium, Release profile, Suspension, Syrup, S-enantiome
Comparative Analysis of Phytochemical and Antioxidative Properties of Different Solvent Extracts of Codium tomentosum Stackhouse for Therapeutic Application
Seaweeds are a phenomenal source of bioactive components in marine environments yet to be explored extensively. The study focused on estimating and identifying phytochemical components, secondary metabolites, and antioxidant efficiency of edible green seaweed Codium tomentosum (Chlorophyta). Qualitative phytochemical analysis of five solvent extracts revealed the presence of Phenol, Flavonoids, Terpenoids, Alkaloids, Tannins, Steroids, Carbohydrates, Glycosides, Amino acids and Proteins. Total phenol content (TPC) equivalent to GAE of five extracts estimated shown highest in chloroform and lowest in methanol - CE (194.53 ± 0.008 mg GAE/g) and ME (138.97 ± 0.007mg GAE/g). Total flavonoid content (TFC) quercetin equivalent (QE) was reported lowest in aqueous extract AE (59.982 ± 0.024 mg QE/g) and highest in chloroform – CE (213.07± 0.014 mg QE/g). The secondary metabolites profile of methanol extract analyzed by GC-MS revealed prominent components, Hexadecanoic acid, Flavones, Oleic acid, Dodecanoic acid, Pentadeconoic acid, and phenol derivative having a spectrum of bioactivity. In vitro, the Antioxidant activity of the five solvent extracts of Codium tomentosum was confirmed by DPPH and ABTS methods. It is evident from the present investigation that the edible green seaweed Codium tomentosum Stack House is a promising source of bioactive components that could be further explored for antimicrobial, anticancer, and antibiofilm properties through green synthesis of nanoparticles for pharmaceutical and nutraceutical applications.
Keywords: Codium tomentosum, phytochemical, GC-MS, anti-oxidative, edible seawee
A Comparative Study on Caprini RAM Vs DOH Tool for Thromboprophylaxis in ICU Setting at Tertiary Care Hospital
The aim of the study was to assess DVT prophylaxis using two models (Caprini RAM & DOH tool) for the prevention of DVT in postoperative or critically ill patients and for better predictability of disease. In this prospective observational study, we compared the Caprini RAM and DOH tool in the ICU setting on 229 patients (140 men and 89 women). 205 patients were considered in the study, out of which 97 had Caprini RAM and 108 had DOH tool. A Prospective, observational comparative study was carried out in a tertiary care hospital for a period of 6 months. Patients were divided into two groups according to the RAM. The data were analyzed using SPSS software and the results were compared using the student t-test. Both GROUP A and GROUP B revealed that the majority of the patients (67.1% & 55.6%) were above 60 years and a large proportion of them required DVT prophylaxis. In GROUP A 93% of forms were complete with 79% accuracy. In GROUP B 83% were complete. The most appropriate prophylaxis received by patients was Enoxaparin sodium 40 mg OD for about 97 (30%) patients and Heparin 5000 IU BD for 108 (30%) based on their Caprini scores and NICE guidelines respectively. The majority of patients in Group A did not require dosage adjustments, but in 20% of cases, it was necessary. Statistical significance was achieved with a p-value less than 0.05. The study demonstrates DOH tool is better than Caprini RAM to be used in hospitals, for risk assessment of VTE in both medical and surgical patients for accuracy and predictability of the prophylaxis.
Keywords: DVT, Risk assessment, Caprini RAM, DOH tool, pharmacological and mechanical Prophylaxis
Formulation and Optimization of Matrix Tablets Based on Spirulina and Vitamin C
Spirulina is a type of algae widely consumed around the world as a dietary supplement due to its great nutritional potential. However, it does not contain vitamin C, a vital vitamin for the proper functioning of the human body, particularly given its immunostimulant potential. The objective of this work was to formulate sustained release spirulina–vitamin C matrix tablets that would enhance particularly a prolonged release and better absorption of vitamin C. A galenic formula based only on vitamin C was made, and then the proportion of vitamin C was reduced in favor of spirulina powder. The manufactured tablets were then subjected to various pharmacopeial quality control tests. The results of these tests showed a good distribution of the powder mixtures in the formulated tablets (i.e., mass uniformity test) and satisfactory outcomes were found for the content uniformity, disintegration and dissolution tests (with 45 % of vitamin C dissolved after 4 hours). Only the results for the friability test were unsatisfactory, indicating the need to improve the physical properties of the powders before compression. These findings open a new area for developing supplementary dietary.
Keywords: Spirulina, Vitamin C, Matrix tablet, Quality control
In-Vitro and In-Silico Approach Distinguish ER-α and HER-2 Antagonistic Properties of Indian Herbal Formulation on Breast Cancer
Objectives: The anticancer effect of an Indian herbal preparation was studied under a cancer cell line, as well as the in silico computational methods that explain the probability of protein ligands binding to ER- α and HER-2 receptors.
Method: The in vitro anticancer activity of Body Revival® suspension (BR) was determined using cytotoxicity tests, cell invasion and migration assays, and metastatic protein expression assays using MCF-7 breast cancer cells. The computational predictive biological method was applied to find out the pharmacodynamic and pharmacokinetic interactions between the active molecules present in the BR and ER- α/and HER-2 of breast cancer.
Results: BR showed significant and dose dependent cytotoxic effects on MCF-7 cells. The 50% effective cytotoxic dose of BR was 34.27µl/ml. It restricted invasion (26%) and migration (28%) of cancer cells than BSA control. MMP-9 and IL-6 concentration were reduced significantly (p<0.001) after treatment. Cucurbitacin B had maximum in silico binding energy score (-7.8) with ER-α, while symconoside B had with HER-2 (-8.4); but, among the other interactions between the two ligands and receptors, withaferin A had the highest affinity (-15.3). Additionally, withaferin A, symconoside A, and symconoside B curcurbitacin A demonstrated bioavailability and fulfilled safety standards.
Conclusion: Body Revival® showed as a powerful multi-target inhibitor of ER- α and HER-2 that has prospective anticancer action without side effects, and may be useful in the therapy management following a successful trial in breast cancer patients.
Keywords: Breast cancer, Cytotoxicity, MCF-7, ER- α, HER-2, Herbs, In Silic
Transdermal Drug Delivery Systems
A transdermal patch is a medicated adhesive patch that is applied to the skin that contains medication that is intended to be absorbed into the bloodstream. This frequently encourages the healing of a body part that has been hurt. Transdermal medication delivery allows for regulated drug release into the patient, resulting in less systemic side effects and, in certain cases, increased efficacy over other dose forms. This is an advantage of transdermal drug delivery over other types of medication delivery such as oral, topical, intravenous, intramuscular, etc. Transdermal medication delivery allows for a constant blood level profile, a regulated drug release into the patient, fewer systemic side effects, and other benefits.
Keywords: Transdermal patch, Blood stream, Systemic side effects
Role of Erythropoietin In Pre-Renal Transplant Patients Undergoing Oral Surgical Procedures-Two Case Reports
The Oral Cavity Is Often Called The "Gateway To The Body," Dentist As The "Gatekeepers Of Health." Chronic Kidney Disease Is An Emerging Disease With Increased Mortality In A Low Resource Setting, According To The Global Disease Burden Report (2015)1 Lack Of Infrastructure And Awareness Among The Public Is Diagnosed At A Late Stage, Leading To Increased Mortality. In A Parallel Line, Dentistry In Developing Countries Still Is An Alien Entity To The Rural And Suburban Areas. End-Stage Renal Failure Patients Who Were Advised For Renal Transplants Visit The Dentist With Poor Oral Hygiene And Foci Of Infection, Which Must Be Eliminated. Anemia In End Stage Renal Disease And Its Management Is Challenging For The Clinicians With The Lack Of Erythropoietin Hormone Exposes The Patients To Risk Of Fatigue, Breathlessness, Lower Quality Of Life And Blood Transfusion2, 3.From Early 1980’s Erythropoesis Stimulating Agents Were Used In Kidney Damaged Patients Undergoing Dialysis But Their Application In Oral Maxillofacial Surgery Was Scarce To Minimize Morbidity And To Avoid Blood Transfusion4-6.
Keywords: Oral Cavity, Chronic Kidney Disease, Dentistry, Oral Hygien
A Systematic Review of Piperine as a Bioavailability Enhancer
Drug oral absorption is a crucial concern, particularly when the medication is costly, poorly bioavailable, and administered for extended periods of time. Chemical substances known as "bioenhancers" are those that, when combined with pharmaceuticals, increase their bioavailability without having a synergistic impact on the drug itself. Toxicity, expense, poor bioavailability, and long-term medication administration all contribute to the need for bioenhancers, which aid in solving the majority of these issues. Piperine, also known as 1-peperoyl piperidine, is an aromatic alkaloid produced by the Piper species. Piperine alters the lipid milieu and membrane dynamics at the site of absorption to improve permeability. The molecular nature of piperine makes it appropriate for inhibiting enzymes. By blocking several metabolising enzymes, it increases the bioavailability of many medications, including carbamazepine, curcumin, ciprofloxacin, ampicillin, metronidazole, oxytetracycline, and many more. As a result, piperine, a potent inhibitor of medication metabolism, effectively increases absorption. The mechanism, metabolic inhibition, influence of structural alterations on activity, and medications that are bioenhanced by piperine are all explored in the review that follows. It offers insight into the use of piperine as a useful bioenhancer and the advantages of a bioenhanced drug formulation over one without one. Bioavailability enhancers are typically plant-based molecules that support the biological activity, bioavailability, or uptake of drugs in combination therapy. This review article finishes with discussing piperine\u27s capacity to increase bioavailability.
Keywords: Bioenhancers, Piperine, Oral absorption, Alkaloid
Pharmacognostical, Phytochemical Screening and Evaluation of Anxiolytic activity of Alcoholic Extract of Withania somnifera (L) Dunal Roots
The roots of Withania somnifera (L) Dunal (W. somnifera) are used extensively in Ayurveda, the classical Indian system of medicine, and W. somnifera is categorized as a rasayana, which are used to promote physical and mental health, to provide defense against disease and adverse environmental factors and to arrest the aging process. W. somnifera has been used to stabilize mood in patients with behavioural disturbances. The objective of this study was to investigate pharmacognostical, phytochemical features and anxiolytic activity of alcoholic extracts of W. somnifera roots. The various pharmacognostical variables were assessed using generally accepted techniques with certain variations. An established test technique that is documented in the literature was used to determine the qualitative analysis of different phytochemical elements. The anxiolytic efficacy of the alcoholic extract of W. somnifera roots in mice was evaluated using the elevated plus maze test (EPMT), light and dark test (L and DT), and open field test (OFT). Extract dosages of 250, 500, and 750 mg/kg were compared to the recommended dosage of diazepam (1 mg/kg) to determine its efficacy. Alcoholic extract underwent phytochemical examination, which identified the presence of fixed oils, lipids, proteins, amino acids, carbohydrates, tannins, and phenolics. The percentage of time spent and the number of entries in the open arm in EPMT were both considerably enhanced by the alcoholic extract of W. somnifera roots (250, 500, 750mg/kg, p.o.). The extract significantly increased time spent, the frequency of crossings, and decreased the length of immobility in the light box in L and DT. The extract in OFT significantly increased the number of rearings, increased ambulation, and decreased self-grooming and faecal dropping all signs of exploratory behaviour. The findings of the current investigation provide scientific support for the traditional use of W. somnifera by indicating that an alcoholic extract of its roots may have anxiolytic properties.
Keywords: Anxiolytic, Withania somnifera (L) Dunal, Elevated plus maze, Open field test, Light and dark tes