Journal of Drug Delivery and Therapeutics (JDDT)
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Development and Evaluation of Microemulsion Formualatons of Valsartan for Solubility Enhancement
Microemulsions have attracted considerable amount of interest as potential drug delivery vehicles largely due to their simple method of preparation, stability and their abilities to incorporate a wide range of drugs of varying solubility. O/W microemulsion is expected to increase the solubility by dissolving low water solubility compounds into its dispersed phase and to enhance the oral bioavailability by protecting the drug increasing the rate of absorption and wettability due to surfactants induced permeability changes and smaller droplet size (< 100 nm) and most importantly able to target lymphatic system.
In the present study, the drug delivery system contains Valsartan, a hydrophilic component, a lipophillic component, surfactants and co-surfactants. The objective is to provide an increased release of valsartan and increased bioavailability of valsartan. Prepared microemulsion formulations by phase-titration method were evaluated for viscosity, drug content, thermodynamic stability studies and in-vitro dissolution. Resultant microemulsion optimized formulation (ME5) shows drug release (88.2±0.16%.%). Hence, micro-emulsion of valsartan was successfully developed and evaluated.
Keywords: Microemulsion, Valsartan, solubility, evaluation
Analytical Review of Medadhatudushti in Prameha
Prameha is a lifestyle disorder, described in ancient medical science. It is a sannipataja disorder having predominance of kaphadosha and medodhatudushti. It is produced by the vitiation of ten dusya which include six dhatu, ojus and body fluids. Among ten dusya meda is prime dusya because of similar nature of kapha and meda. Various factors i.e. aharaja and viharaja nidana, increase kapha dosha which in turn vitiates medodhatu. Vitiated kapha affects the medovahasrotasa and medodharakala. Medadhatwaagni gets degraded resulting into improper formation of medadhatu. The abnormal medadhatu is responsible for obesity and prameha. It leads to the manifestation of many purvarupa of prameha & ultimately prabhutaavila mutrata. Assessment of medadusthi is very important for the early diagnosis and proper treatment of prameha.
Keywords: Prameha, Medadhatu, Medadhatwaagni, Medadhatudusht
The Relationship between Physical Activity and Body Mass Index During the Covid-19 Pandemic in Students of the Faculty of Medicine, Indonesian Christian University
Background: Policies related to large-scale restrictions during the pandemic require each individual to carry out physical activities and routines at home, so every activity that is usually carried out is now completely limited, and it affects the current public health, as well as there is no research related to the relationship between physical activity and BMI in the 2018 batch of the Faculty of Medicine, Christian University of Indonesia. It is the basis of researchers conducting this research. Method: This research design is descriptive-analytic, with a cross-sectional approach, with a population of 156 respondents and a sample of 113 respondents whom Spearman will analyze with a p-value < 0.05. Result: The frequency of physical activity in the 2018 Indonesian Christian University Faculty of Medicine students in the "Light" category was 54% (61 people), "Medium" was 30.1% (34 people), and "Heavy" was 15.9% (18 people). Meanwhile, the frequency of Body Mass Index in the respondents in this study was divided into the categories of "undernourished" by 11.5% (13 people), "Normal" by 63.7% (72 people), "Overweight" by 9.7% (11 people), and "Obesity" by 15% (17 people). Then, both were correlated with a significant value of 0.04. Conclusion: The Body Mass Index in the 2018 Indonesian Christian University Faculty of Medicine students was in the normal category at most 63.7% (72 people), while the most physical activity was, the light category was 54% (61 people), and these two variables had a correlation one another.
Keywords: Physical Activity, BMI, Covid 19 Policy, Health, Restrictio
Formulation Development and In-Vitro Evaluation of Transferosomal Gel of Mometasone Furoate
The main aim of the study is to formulate and evaluate transferosomal gel formulation for effective topical delivery of Mometasone furoate. The transferosomes was prepared using thin film hydration technique by various proportions of Soya phosphatidylcholine, tween 80. The drug was encapsulated into eight different Transferosomal formulations from F1-F8. The optimized formulation F4 showed small particle size (152.48 nm), entrapment efficiency % EE of 87.16%, zeta potential of -32mV, 0.252 PDI and % Cumulative Drug Release of (97.14%). SEM of optimized Transferosome appeared as spherical, well identified, Unilamellar vesicles. The optimized formulation of Transferosomes was further formulated to transferosomal gel with Carbopol-940 (0.2 to 0.8% w/w), HPMC k15 (0.2 to 0.8% w/w), Propylene glycol, Triethanolamine and Isopropyl alcohol. Among these, F4 formulation with Carbopol-940 0.8%w/w transferosomal gel is the optimized transferosomal gel and showed Spreadability value 0.229±0.01gm.cm/sec, pH value 5.8. The actual drug content of the Transferosomal gel was found to be 98.90%, which represents good content uniformity. The viscosity of optimized Transferosomal gel was found to 55417cps. The percentage drug release for Transferosomal gel was 98.22%. And the formulation was stable throughout the stability studies. This research suggests that Mometasone Furoate loaded transferosomal gel can be potentially used as a transdermal drug delivery system for effective topical delivery.
Keywords: Mometasone Furoate, Transfersomes, Soya phosphatidyl choline and Tween 80
Revolutionizing Drug Delivery: Nicardipine Nanosuspension Formulation and In-Vitro Evaluation
Nicardipine hydrochloride, is a potent calcium channel blocker, is commonly used in the management of hypertension and angina. It is a BCS class II drug which has low aqueous solubility and high permeability. In the present study, an attempt was made to formulate and evaluate nanosuspension of Nicardipine hydrochloride using different stabilizers, namely Tween 80, PVP K30, Poloxamer 188 by using Nanoprecipitation method with the objective to improve solubility and enhance dissolution of Nicardipine hydrochloride. Prepared nanosuspensions were evaluated for drug-excipient compatibility, particle size, PDI (Polydispersity Index), Zeta potential, Drug content, Saturation solubility, In-vitro release study, Scanning electron microscopy (SEM). FTIR (Fourier Transform Infrared Spectroscopy) studies revealed the compatibility of the drug with excipients. Nanosuspension (F3), which had the lowest particle size and the highest % Drug Release, was selected as the optimum formulation. It showed the droplet size, PDI, ZP,% Drug content and %Drug release of 150.4 nm,0.243, -30.6 mV,95.52%,91.24%. Kinetic release profiles of the NS F3 revealed that it followed First order kinetics. This study showed the ability of nanosuspension system in improving the solubility and drug release of Nicardipine.
Keywords: Nicardipine, Nanosuspension, Solubility, % Drug Release, % Drug content, Scanning electron microscopy
Phytochemistry and Antiperoxidative Potential of Cannabis sativa L. Leaves Methanol Extracts: An In Vitro Study
Aim: Present study aimed to demonstrate the preliminary phytochemical composition, antioxidant and in vitro protective potential of the methanolic extract of Cannabis sativa L.
Study Design: A methanolic extract of Cannabis sativa L. leaves was prepared and assessed at the in vitro level for its preliminary phytochemical screening and antiperoxidative potentials by using the DPPH radical reduction assay, lipid peroxidation inhibitory activity, protein carbonyl inhibitory potential in glycated bovine serum albumin, and enzyme antioxidant activity in a goat liver homogenate system exposed to hydrogen peroxide as oxidant molecule.
Results: The methanolic extract of Cannabis sativa L. leaf contained a diverse range of phytoconstituents, including alkaloids, flavonoids, tannins, terpenoids, and saponins. Upon quantitative analysis, the methanolic extract of C. sativa L. reflected 50 ± 0.013 µg quercetin equivalent / mg of extract according to the querecetin standard graph, while 28.03 ± 0.024 % alkaloid content was retrieved after quantification.
Conclusion: We suggest that, upon tested on all in vitro antioxidant parameters; the leaf methanolic extract of Cannabis sativa L. demonstrated potent antioxidant and protective activity.
Keywords: Cannabis sativa L., Antioxidant, in vitro, DPPH, LPO, Protein carbonyl, peroxidative potentia
An Improved Cell Culture Process for Production of Omalizumab
The demand for biopharmaceutical products such as monoclonal antibodies (MAbs), fusion proteins, viral vaccines, and hormones is rapidly increasing. Mammalian cell cultures with ease of process operations are adopted to get the desired product. The challenges of low productivity and impurities in the desired product can be eliminated by optimizing the process parameters. The present study focuses on the optimization of temperature with other parameters to achieve improved titer and reduced heterogeneity in Omalizumab. An anti-IgE antibody expressed in mammalian cell culture. It is noticed that maintaining a specific temperature of 36.5° C ± 0.5 and pH 6.8± 0.1 during fed-batch cell culture provides improved quality (reduced galactosylation and reduced acidic variants) and quantity (improved titer) of the Omalizumab.
Keywords: antibody, omalizumab, mammalian cells, acidic variant
Immediate-release dosage form; focus on disintegrants use as a promising excipient
Disintegrants are materials or mixtures of substances added in the drug formulations, which make easier dispersion or breakup of tablets and ingredients of capsules in small-scale particles for fast dissolution then it comes in contact with water in the GI tract. Immediate drug release dosage forms disintegrate rapidly after administration with an enhanced rate of dissolution. The superdisintegrants provide instantaneous disintegration of tablets after administration in the stomach. In this field, immediate-release liquid dosage forms and parenteral dosage forms have also been introduced for treating patients. The oral route is the most convenient route for the administration of solid dosage form, about 85% of solid dosage is administered by the oral route because of its advantages over others. The therapeutic activity of these formulations is obtained through a typical manner like disintegration followed by dissolution. Hence disintegration has a major role in facilitating drug activity. Diverse categories of superdisintegrants such as synthetic, semi-synthetic, natural, co-processed blends, multifunctional superdisintegrants, etc. have been employed to develop effectual orodispersible tablets and to overcome the limitations of conventional tablet dosage forms. The objective of the present review article is to highlight the various kinds of traditional, Natural crude drugs containing gum and mucilage, Co-processed, semisynthetic and synthetic disintegrants along with a concentration in tablet and capsule disintegration and effect on drug release, which are being used in the formulation to provide the safer, effective drug delivery with patient compliance. Also highlights the mechanism and use of disintegrants in the immediate release dosage form.
Keywords: Disintegrants, Natural, Co-processed, Immediate releas
Antibacterial and antifungal activity of Combretum farinosum Kunth and Combretum igneiflorum Rendón & R. Delgad. extracts
Infectious diseases like bacterial, fungal, viral are the top killers of a third of the world population. Limited access to comprehensive treatment forces people to rely on herbal concoctions for treatment. Combretum farinosum Kunth and C. igneiflorum Rendón & R. Delgad. are two similar vine plant species that have insufficient scientific investigation. The purpose of the study is to determine the in vitro antimicrobial activity of crude extracts of different parts of Combretum igneiflorum (roots, stem, and leaves) and Combretum farinosum (roots, fruits, leaves, and stem) using petroleum ether, acetone, and ethanol-water. The crude extract was tested against food-borne pathogens. Twenty-seven crude extracts were prepared from C. igneiflorum (roots, stem, and leaves) and C. farinosum (roots, stem, leaves, and fruits) and screened for their antimicrobial activity against four Gram-positive bacteria (Enterococcus faecalis, Staphylococcus aureus, Staphylococcus aureus methicillin resistant, Bacillus subtilis), four Gram-negative bacteria (Salmonella enteritidis, Pseudomonas aeruginosa, Shigella flexneri, and Escherichia coli B), and one fungus species (Candida albicans) using agar disc-diffusion, and microbroth dilution assays. Results show that crude extracts of both plants tested had broad antimicrobial activity. The minimum inhibitory concentration (MIC) of C. farinosum extract against tested bacteria ranged from 0.32 to 100 mg/ml, whereas C. igneiflorum extracts that showed antibacterial activity ranged from 2.5 to 75 mg/ml. Gram-positive bacteria tested were more susceptible to the extracts than gram-negative bacteria. Crude extracts of C. igneiflorum and C. farinosum have broad antimicrobial activity against the microbes tested.
Keywords: Combretum farinosum Kunth, Combretum igneiflorum Rendón & R. Delgad. MTT, Minimum Inhibitory Concentration (MIC), Antifungal, Antibacterial
Methanolic and ethanolic phytochemical screening of Sweet flag (Acorus calamus L.) rhizome
Acorus calamus is a medicinal plant with several ethno-medicinal properties. The present study was carried to screen the presence of major phytochemical groups. Phytochemical screening of methanolic and ethanolic rhizome extract showed the presence of carbohydrates, alkaloids, phenolic compound, protein, amino acid flavanoids and tannins. The total phenolic content in methanolic and ethanolic rhizome extracts in terms of gallic acid equivalent was 4.77.50 and 7.5 mg/g of extract powder respectively whereas the total flavonoid content of methanolic and ethanolic extract was 12.02 and 12.89 mg QE/g of extract respectively. Total antioxidant activity was found highest in ethanol extract (75.6 µg AAE/mg of extract) than methanol extract (37.2 µg AAE/mg of extract). Reducing power is also found highest in ethanol extract than methanol extract.
Keywords: Acorus calamus, phytochemical screening, methanol, ethanol