Garuda - Garba Rujukan Digital

Optimizing novasomes: impact of oleic acid and co-surfactant ratio on posaconazole delivery: In vitro & Ex vivo pharmacokinetic study Rukari, Tushar; Pingale, Prashant L; Upasani, Chandrashekhar D
Journal of Applied Pharmaceutical Research Vol. 12 No. 3 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i3.536

Background: Posaconazole, currently available as a solid oral dosage form, possesses erratic pharmacokinetics that complicate dosing regimens and increase the risk of adverse effects and drug interactions. Hence, innovative strategies, especially topical ones, are necessary to enhance the therapeutic profile and improve patient outcomes. Methodology: The regular 23 factorial design and the concentrations of Oleic acid: Span 80 (2:1) ratio, Cholesterol, and Tween 80 as independent variables were used for the formulation development. The preliminary effect was determined by dependent variables like vesicle size and entrapment efficiency; then the final optimized batch was loaded in 3 % w/w Carbopol gel. Result and Discussion: The optimized batch's vesicle size and entrapment efficiency were 193.34+14.84 nm and 90.03+0.11 %, respectively. These results were found statistically significant (ANOVA) in the trial version of Stat-Ease 360®. Other evaluation parameters like zeta potential and pH of all the formulations were also significant (p<0.005). Conclusion: The optimized batch (NF7), when loaded with gel (NF7G-3), showed sustained release of Posaconazole up to 7 h in an In vitro diffusion study facilitated 87.14±0.11 % release confirming non-Fickian or Anomalous diffusion, interpreted from Korsmeyer Peppas (KKP) model. With the results from In vitro and Ex vivo pharmacokinetic release, the Posaconazole-loaded NF7G-3 Novasomal gel can exhibit potential formulation for the topical treatment of fungal infections. It will help significantly mitigate the negative effects of Posaconazole.

Pharmaceutical development of etodolac transfersomal gel for topical drug delivery system in rheumatoid arthritis Bachhav, Ashwini; Pingale, Prashant L; Upasani, Chandrashekhar D
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.597

Background: Transferosomes provide delivery of the drug into systemic circulation via the skin as a topical delivery system. So, this study started with the objective of formulating Etodolac transfersomal gel to enhance its skin permeation. Methodology: A total of nine transferosomes (ET-1 to ET-9) containing lecithin, different grades of span and tween, were successfully prepared using a rotary film evaporator. Results and Discussion: After primary evaluation, results were as particle sizes ranged from 222 to 421 nm, zeta potential shows results from –18.50 to –62.53 mV with PDI values 0.254 to 0.303, and the entrapment efficiency (EE%) of Etodolac in the transferosomes ranged from 54.15% to 80.25%. Additionally, the transfersomes formulations were included in carbopol 940 gels (ETC-1 to ETC-9 and EC-0 without transferosomes) and assessed for various characteristics like color, pH, homogeneity, spreadability, viscosity, and in vitro drug release study. Optimized formulation (ET4 and ETC4) underwent further analysis using SEM, TEM, DSC, FTIR, XRD, ex vivo skin permeation, skin irritation and in vivo studies. The in vivo results were compared. % edema inhibition maximum was observed with optimized transfersomal gel formulation (ETC4) as compared to the marketed formulation and plain Carbopol gel when the study was completed after 8 hrs. Conclusion: After this research, it is suggested that Etodolac Transfersomal gel (ETC4) can be considered as an alternate drug carriers system for topical delivery and it could be used to treat Rheumatoid Arthritis

Formulation and evaluation of phytosomes containing bioactive from Carica papaya seeds Patil, Rima R; Pingale, Prashant L; Upasani, Chandrashekhar D
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.622

Background: Papaya seeds are a rich source of proteins, fat, fibers, vitamins, minerals, monounsaturated fatty acids, polyphenols, and powerful antioxidants like flavonoids. Low solubility limits the absorption and bioavailability of herbal constituents. Hence, phytosomes of Papaya seed extract were formulated to enhance its solubility and bioavailability. Methodology: Papaya seeds were extracted using ethanol as solvent, and all the phytoconstituents present in the extract were assessed during the phytochemical screening and LC-MS analysis. In-vitro antidiabetic activity pure extract was determined by alpha-amylase and alpha-glucosidase enzyme inhibitory assay. The phytosomes of extract were formulated using the lipid thin film formation method and Soya lecithin and Cholesterol as lipids. The formulated phytosomes were analyzed for parameters such as particle size, zeta potential, encapsulation efficiency, percent drug content, and In-vitro dissolution study. The chemical nature of the formulation was studied using FTIR analysis and powder X-ray diffractometry. Thermal stability of phytosomes analyzed with the help of Differential Scanning calorimetry. Results: LC-MS identified 16 phytoconstituents. In-vitro antidiabetic activity showed 59.97% and 51.17% inhibition of enzymes alpha-amylase and alpha-glucosidase, respectively. The encapsulation efficiency of the optimized formulation was 88.41±0.91% with a particle size of 188.0±53.7nm. TEM images of formulation confirm the formation of phytosomes. FTIR, DSC, and Powder X-ray diffractometry showed no unwanted peaks. The in vitro dissolution study showed 89.26±1.05% CDR of phytosome, while the extract showed 47.78±0.59% CDR. Conclusion: Evaluation results of phytosomes suggest that this formulation can be used as an effective herbal antidiabetic formulation

In vitro evaluation of Punica granatum fruit peel extract for its potential anti-diabetic effects More, Rutuja K; Pingale, Prashant L; Upasani, Chandrashekhar D; Amrutkar, Sunil V
Journal of Applied Pharmaceutical Research Vol. 12 No. 6 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i6.739

Background: With growing awareness of pomegranate's health benefits, pomegranate products have been consumed more frequently in recent years, and pomegranate peel has emerged as one of the most prevalent wastes in the food industry. Pomegranate Peel concentrate is an indigenous substance with strong antioxidant and antidiabetic actions as a result of its tannins as well as polyphenols content. Methods: In the present study, pomegranate skin extract, both liquid and alcohol-based, was evaluated for polyphenolic and flavonoid content. Alcoholic fruit peel extract was also assessed for 1,4-α-D-glucan glucanohydrolase and α-D-glucoside glucohydrolase enzyme activity. Results: According to findings, pomegranate peel extract showed significant antioxidant content. Phytochemical analysis of ethanol-derived extract of pomegranate peel found a noteworthy amount of ellagitannins and flavonoids such as Punicalin, Punicalgin, Punicic acid, Catechin, Quercetin, Rutin, and Kaempferol. In contrast, punicalgin, ellagic acid, and gallic acid are responsible for antidiabetic activity. The LC-MS characterization of peel extract of pomegranate showed 10 bioactive compounds. The IC50 value for 80% alcoholic extract of pomegranate peel was found to be 5.86 mg/ml of α- amylase and 6.58 mg/ml of α-glucosidase. Conclusion: It was found that the inhibition of 1,4-α-D-glucan glucanohydrolase and α-D-glucoside glucohydrolase enzymes could be an effective mechanism by which it can give anti-diabetic effects.

Title

Found 4 Documents
Search

Abstract

Abstract

Abstract

Abstract

Title Search

Found 4 Documents Search

Abstract

Abstract

Abstract

Abstract

Title

Found 4 Documents
Search