Development of a Prolonged-Release Pramipexole Transdermal Patch: In Vitro and In Vivo Evaluation

In this study, poly(hydroxybutyrate-co-hydroxyvalerate) (PHBV) and poly(l-lactide) (PLA) microspheres containing ibuprofen were prepared with the aim of prolonging the drug release. The oil-in-water (O/W) emulsion solvent evaporation technique was used, varying the polymer ratio. All formulations provided spherical particles with drug crystals on the surface and a porous and rough polymeric matrix when PHBV was used and smooth external surface when prepared with PLA. The in vitro dissolution profiles show that the formulation containing PHBV/PLA at the proportion of 30/70 presented the best results in terms of prolonging the ibuprofen release. The analysis of the concentration of ibuprofen in the blood of rats showed that maximum levels were achieved at between one and two hours after administration of the immediate-release form (pure drug), while the prolonged microspheres led to a small amount of the drug being released within the first two hours and reached the maximum level after six hours of administration. It was concluded that it is possible to prolong the release of ibuprofen through its incorporation into PHBV/PLA microspheres.

Download Full-text

EVALUASI IN VITRO-IN VIVO FILM TRANDERMAL DILTIAZEM HCL DENGAN PENINGKAT PENETRASI PEG 400 SEBAGAI ANTIHIPERTENSI

JIFFK : Jurnal Ilmu Farmasi dan Farmasi Klinik ◽

10.31942/jiffk.v16i01.2922 ◽

2019 ◽

Vol 16 (01) ◽

pp. 1

Author(s):

Yulias Ninik Windriyati ◽

Risha Fillah Fithria ◽

Fitria Dwi Kurniawati ◽

Ulfa Risalatul Mukaromah

Keyword(s):

Blood Pressure ◽

Physicochemical Characteristics ◽

Penetration Enhancer ◽

Transdermal Patch ◽

In Vivo Evaluation ◽

Peg 400 ◽

Transdermal Patches ◽

Diltiazem Hcl

ABSTRACTDiltiazem HCL is an antihypertensive that low oral bioavailability of 40%, so developed to transdermal preparations. A matrix type of transdermal patch of diltiazem HCl was prepared using polyvinyl alcohol and ethyl cellulose with PEG 400 as penetration enhancer. In vitro-in vivo evaluation were conducted to asses drug permeation through the skin and determine the effectiveness of transdermal film as an antihypertensive drug. Transdermal patches of diltiazem HCl were evaluated for physicochemical characteristics weight variation, thickness, folding endurance, moisture uptake, and drug content. In vitro permeation study was conducted using commercial semi permeable membrane in Franz diffusion cell. In vivo activity study was evaluated on male rat Wistar that induced NaCl with CODA non-invasive blood pressure method. Transdermal patches of diltiazem HCl were found no significant differences in terms of physicochemical characteristics. The in vitro skin permeation profiles showed increased flux values with the increase of PEG 400 as a penetration enhancer. The in vivo evaluation showed a reduction in systolic and diastolic blood pressure within one hour after the drug administration. Diltiazem HCl was able penetration into skin, absorbed in blood circulation and effective as antihypertensive via transdermal route.Keywords : antihypertension, diltiazem HCl, PEG 400, transdermal patch

Download Full-text

In vitro and in vivo evaluation of the anti-inflammatory effects of Arzanol from Helichrysum italicum

Planta Medica ◽

10.1055/s-0030-1264369 ◽

2010 ◽

Vol 76 (12) ◽

Author(s):

J Bauer ◽

F Dehm ◽

A Koeberle ◽

F Pollastro ◽

G Appendino ◽

...

Keyword(s):

In Vivo Evaluation ◽

Anti Inflammatory

Download Full-text

Faculty Opinions recommendation of A fluoroacetamidine-based inactivator of protein arginine deiminase 4: design, synthesis, and in vitro and in vivo evaluation.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1031506.367705 ◽

2006 ◽

Author(s):

Karen Allen

Keyword(s):

Arginine Deiminase ◽

In Vivo Evaluation ◽

Design Synthesis ◽

Protein Arginine Deiminase

Download Full-text

Faculty Opinions recommendation of In vitro and in vivo evaluation of a novel oral insulin formulation.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1046627.496622 ◽

2006 ◽

Author(s):

Marival Bermejo

Keyword(s):

Oral Insulin ◽

In Vivo Evaluation ◽

Insulin Formulation

Download Full-text

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2020.13.5.7 ◽

2020 ◽

Vol 13 (5) ◽

pp. 5102-5109

Author(s):

Venu Madhav K ◽

Somnath De ◽

Chandra Shekar Bonagiri ◽

Sridhar Babu Gummadi

Keyword(s):

Oral Bioavailability ◽

Oral Delivery ◽

Solid Dispersions ◽

In Vitro Release ◽

Aqueous Solubility ◽

Water Soluble ◽

Scanning Calorimetry ◽

In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension. From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

Download Full-text

Design and In vivo Evaluation of Palonosetron HCl Mouth Dissolving Films in the Management of Chemotherapy-Induced Vomiting

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2017.10.6.9 ◽

2017 ◽

Vol 10 (6) ◽

pp. 3929-3936

Author(s):

Y. Srinivasa Rao ◽

K. Adinarayana Reddy

Keyword(s):

Drug Release ◽

Patient Compliance ◽

Onset Of Action ◽

In Vivo Evaluation ◽

Disintegration Time ◽

In Vitro Drug Release ◽

Surface Ph ◽

Drug Content

Fast dissolving oral delivery systems are solid dosage forms, which disintegrate or dissolve within 1 minute in the mouth without drinking water or chewing. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use and the consequent patient compliance. The purpose of this work was to develop mouth dissolving oral films of palonosetron HCl, an antiemetic drug especially used in the prevention and treatment of chemotherapy-induced nausea and vomiting. In the present work, the films were prepared by using solvent casting method with various polymers HPMC E3, E5 & E15 as a film base synthetic polymer, propylene glycol as a plasticizer and maltodextrin and other polymers. Films were found to be satisfactory when evaluated for thickness, in vitro drug release, folding endurance, drug content and disintegration time. The surface pH of all the films was found to be neutral. The in vitro drug release of optimized formulation F29 was found to be 99.55 ± 6.3 7% in 7 min. The optimized formulation F29 also showed satisfactory surface pH, drug content (99.38 ± 0.08 %), disintegration time of 8 seconds and good stability. FTIR data revealed that no interaction takes place between the drug and polymers used in the optimized formulation. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Palonosetron Hydrochloride. Therefore, the mouth dissolving film of palonosetron is potentially useful for the treatment of emesis disease where quick onset of action is desired, also improved patient compliance.

Download Full-text

Formulation and In Vivo Evaluation of Mucoadhesive Micro-spheres of Rebamipide, a Mucoprotective Drug for GIT Disorders

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2018.11.3.2 ◽

2018 ◽

Vol 11 (3) ◽

pp. 4089-4097

Author(s):

Bhikshapathi D. V. R. N. ◽

Kanteepan P

Keyword(s):

Drug Release ◽

Entrapment Efficiency ◽

In Vivo Studies ◽

Amino Acid Derivative ◽

Release Mechanism ◽

In Vivo Evaluation ◽

In Vitro Drug Release ◽

Percentage Yield

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.

Download Full-text