scholarly journals Development of Buccoadhesive Systems of Pentarocine for Systemic Drug Delivery

2003 ◽  
Vol 71 (4) ◽  
pp. 281-301
Author(s):  
D. Sampathkumar ◽  
M. Thilek Kumar ◽  
J. Balasubrarnaniam ◽  
J. Pandit
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Propylene Glycol ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Zero Order ◽  
Healthy Human ◽  
Human Volunteers

Bucoadhesive patches of Pentazocine (PZ) for unidirectional drug delivery were prepared by casting carboxy methyl cellulose (CMC) with glycerol or propylene glycol and CMC-hydroxy ethyl cellulose (HEC) with glycerol. In vitro mucoadhesivity of the prepared patches were determined using a modified mucoadhesive bond strength apparatus using rabbit small intestine mucosa (SIM). Drug release kinetics was evaluated from composite patches, prepared by covering all but one side of the PZ patches with 3M backing material. Biocompatability / buccoadhesion time and in vivo permeation of placebo and PZ loaded patches were determined using a double blind cross over study in healthy human volunteers. Drug release from CMC-glycerol patches and pure HEC patches showed zero order kinetics with diffusional exponent (n) ranging between 0.79 to 1.046, while that from CMC-HEC and CMC-propylene glycol patches showed an apparent zero order release kinetics. The prepared patches were well tolerated by the human volunteers as they did not produce any side effects at the contact surface. The in vitro mucoadhesivity of CMC-propylene glycol patches were significantly lower than CMC- glycerol based patches. The in vivo permeation of selected PZ patches delivered the drug well above the minimum buccal permeation rate, so as to attain effective blood concentration

Gastroretentive Floating Capsules of Risedronate Sodium: Development, Optimization, in vitro and in vivo Evaluation in Healthy Human Volunteers

2015 ◽  
Vol 8 (2) ◽  
pp. 2835-2842
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Arun Kumar Jarathi ◽  
Suresh Gande ◽  
Viswaja Medipally ◽  
Ramesh Bomma
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Zero Order ◽  
Wet Granulation ◽  
Capsule Formulation ◽  
In Vivo Evaluation ◽  
Healthy Human ◽  
X Ray ◽  
Human Volunteers

Background and the purpose of the study: Risedronate sodium inhibits osteoclast bone resorption and modulates bone metabolism. Risedronate has a high affinity for hydroxyapatite crystals in bone and is a potent antiresorptive agent. In the present investigation efforts were made to improve the bioavailability of risedronate sodium by increasing the residence time of the drug through sustained-release matrix capsule formulation via gastroretentive mechanism. Capsules were prepared by wet granulation technique. The influence of gel forming agents, amount of risedronate and total weight of capsules on physical properties, in vitro buoyancy, drug release, FTIR, DSC, X-ray studies were investigated. The release mechanisms were explored and explained by applying zero order, first order, Higuchi and Korsmeyer equations. The selected formulations were subjected to stability study at 40 °C/75% RH, 25 °C/60% RH for the period of three months. For all formulations, kinetics of drug release from capsules followed Higuchi’s square root of time kinetic treatment heralding diffusion as predominant mechanism of drug release. Formulation containing 25 mg HPMC K4M and 75 mg HPMC K100 LV (F-8) showed zero order release profile. There was no significant change in the selected formulation, when subjected to accelerated stability conditions over a period of three months. X-ray imaging in six healthy human volunteers revealed a mean gastric retention period of 5.60 ± 0.77 hrs for the selected formulation. Stable, sustained release effervescent floating capsules of risedronate sodium could be prepared by wet granulation technique.  

scholarly journals COMPARATIVE EVALUATION OF SELECTED POLYMERS AND PLASTICIZER ON TRANSDERMAL DRUG DELIVERY SYSTEM

2018 ◽  
Vol 10 (1) ◽  
pp. 67
Author(s):  
Bhawana Sethi ◽  
Rupa Mazumder
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Propylene Glycol ◽  
Drug Delivery System ◽  
Transdermal Drug Delivery ◽  
Release Kinetics ◽  
Content Uniformity ◽  
Transdermal Drug Delivery System ◽  
Transdermal Patches

Objective: The present work was aimed at preparation of transdermal patches by a solvent casting method using a varying concentration of polymers i.e. methocel (K15 and K100), ethocel (4 and 10), gelatin, chitosan, eudragit (RL and RS) grade using plasticizer (glycerin and propylene glycol).Methods: The ratio of drug to polymers and plasticizer was varied and the effect of formulation variables was studied. Prepared transdermal patches were evaluated for physicochemical properties, in-vitro permeation studies, content uniformity, primary skin irritation studies and FT-IR studies.Results: The formulated transdermal patch by using Methocel K 100 M showed good physical properties. The average weight of patches prepared using glycerin as a plasticizer were ranged from 42.33-67.00 mg and propylene glycol as a plasticizer were ranged from 40.67-67.67 mg. The percentage moisture absorption varies from 1.76 to 10.73 for patches formulated using glycerin and 2.28 to 7.97 for propylene glycol patches. The percentage moisture loss from patches prepared using glycerin was ranged from 2.75 to 11.54 and 2.87 to 12.02 from propylene glycol. The water vapour transmission rate from patches prepared using glycerin was ranged from 0.25 to 0.92 and 0.41 to 1.76. The formulated patch showed the acceptable quantity of medicament ranged from (100.20-101.05%). This result met the test content uniformity as per BP (85% to 115%). According to that, the drug was consistent throughout the patches. The formulation PGD is considered as the best formulation, since it shows a maximum in vitro drug release as 43.75 % at 24 h. The drug release kinetics studied showed that the majority of formulations was following zero order.Conclusion: In conclusion, controlled release transdermal drug delivery system patches of aliskiren can be prepared using polymer combinations, with a different plasticizer. The release rate of drug depends upon the polymer. However, release kinetics followed zero order.

scholarly journals Laser-activated drug implant for controlled release to the posterior segment of the eye

2020 ◽  
Author(s):  
Xingyu He ◽  
Zheng Yuan ◽  
Samantha Gaeke ◽  
Winston W.-Y. Kao ◽  
S. Kevin Li ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Posterior Segment ◽  
Zero Order ◽  
First Order ◽  
Drug Implants

AbstractThe current standard of care for posterior segment eye diseases, such as age-related macular degeneration and diabetic macular edema, is frequent intravitreal injections or sustained-release drug implants. Drug implants have side effects due to the burst release of the drugs, and their release cannot be easily controlled after implantation. Present study attempts to develop a dosage-controllable drug delivery implant which consists of a nanoporous biodegradable PLGA capsule and light-activated liposomes. Controllable drug release from the implant was achieved by using pulsed near-infrared (NIR) laser both in vitro and in vivo. The in vitro drug release kinetics from two different initial dose implants, 1000 μg and 500 μg, was analyzed by fitting zero order and first order kinetics, as well as the Korsmeyer-Peppas and Higuchi models. The 1000 μg and 500 μg implants fit the first-order and zero-order kinetics model, respectively, the best. The multiple drug releases in the vitreous was determined by in vivo fluorimeter, which was consistent with the in vitro data. The dose released was also clinically relevant. Histology and optical and ultrasound imaging data showed no abnormality in the eyes received implant treatment suggesting that the drug delivery system was safe to the retina. This on-demand dose-controllable drug delivery system could be potentially used for long-term posterior eye disease treatment.

Design and in vivo Evaluation of Gastro-retentive Floating Capsules of Amlodipine Besylate in Healthy Human Volunteers

2017 ◽  
Vol 10 (6) ◽  
pp. 3891-3899
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Chenna Madipalli Shalina ◽  
Vishnu Pulavarthy ◽  
Viswaja Medipally
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
In Vivo Studies ◽  
Amlodipine Besylate ◽  
In Vivo Evaluation ◽  
Healthy Human ◽  
Gastro Retentive

The aim of this study was to explore the application of Gelucire 43/01 for the design of sustained release gastro retentive drug delivery system of Amlodipine besylate. Gelucire 43/01 has been used in floating sustained release formulations to prolong gastric residence time and increase its bioavailability. Gelucire 43/01 in combination with HPMC and Polyox was used as a release retarding polymer. HPMC of various viscosity grades HPMC K4M, HPMC K15M and HPMC K100M in combination of Gelucire were tested to obtain optimal total floating time as well as controlled drug release for prolonged period. Melt granulation technique has been used to prepare gastro retentive Amlodipine besylate formulations. All the formulations were evaluated in vitro for their floating ability and drug release. The floating times of all tablet formulations were greater than 12h. HPMC K4M in combination with Gelucire as polymeric matrix enhanced the drug release due to addition of hydrophilic polymer facilitated the swelling and erosion of the tablets. Incorporation of low viscosity polymer HPMC K100 M resulted in optimal floating as well as drug release for longer time. In vivo studies of optimized formulation show floating ability for 6 h in stomach. The results indicate that Gelucire 43/01 in combination with dissolution enhancers HPMC increase the permeability of the wax matrix, which provides improved dissolution thereby bioavailability of Amlodipine besylate and can be considered as a carrier for the development of sustained release floating drug delivery systems.  

Development of Multiple-Unit Floating Drug Delivery System of Clarithromycin: Formulation, in vitro Dissolution by Modified Dissolution Apparatus, in vivo Radiographic Studies in Human Volunteers

Drug Research ◽  
2017 ◽  
Vol 67 (07) ◽  
pp. 412-418 ◽  
Author(s):  
Arun Reddy ◽  
Narendar Reddy
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Release Kinetics ◽  
In Vitro Dissolution ◽  
Physical Parameters ◽  
Gastric Residence Time ◽  
Human Volunteers ◽  
Multiple Unit

AbstractClarithromycin (CM), a broad spectrum macrolide antibiotic used to eradicate H. pylori in peptic ulcer. Clarithromycin (CM) is well absorbed from the gastrointestinal tract, but has a bioavailability of 50% due to rapid biodegradation. The aim of this investigation was to increase the gastric residence time, and to control the drug release of clarithromycin by formulating into multiple unit floating mini-tablets. Floating tablets were prepared by using direct compression method with HPMC K4M and Polyox WSR 1105 as release retarded polymers and sodium bicarbonate as gas generating agent. The prepared mini-tablets were evaluated for thickness, weight variation, friability, hardness, drug content, in vitro buoyancy, swelling studies, in vitro dissolution studies by using modified Rossett-Rice test and in vivo radiographic studies in healthy human volunteers in fasting conditions. DSC analysis revealed that no interaction between drug and excipients. All the physical parameters of the tablets were within the acceptable limits. The optimized formulation (F6) had showed controlled drug release of 99.16±3.22% in 12 h, by zero-order release kinetics, along with floating lag time of 9.5±1.28 s and total floating time of 12±0.14 h. X-ray imaging studies revealed that in vivo gastric residence time of clarithromycin floating mini-tablet in the stomach was about 3.5 h. The results demonstrated that the developed floating mini-tablets of clarithromycin caused significant enhancement in gastric retention time along with sustained effect and increased oral bioavailability.

Drug Release and Pharmacokinetic Evaluation of Novel Implantable Mometasone Furoate Matrices in Rabbit Maxillary Sinuses

2021 ◽  
pp. 194589242110391
Author(s):  
Changcheng You ◽  
Ling-Fang Tseng ◽  
Alexander Pappas ◽  
Danny Concagh ◽  
Yina Kuang
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Kinetics ◽  
Mometasone Furoate ◽  
In Vitro Drug Release ◽  
Nasal Sprays ◽  
Maxillary Osteotomy ◽  
Maxillary Sinuses

Background Intranasal corticosteroid sprays (INCSs) used to treat chronic rhinosinusitis are suboptimal due to limited penetration into the middle meatus, rapid clearance, and poor patient compliance. A bioresorbable drug matrix, developed with the XTreoTM drug delivery platform, may overcome the limitations of INCS by providing continuous dosing over several months. Objective To evaluate the in vitro drug release and in vivo pharmacokinetics of novel mometasone furoate (MF) matrices in a rabbit dorsal maxillary osteotomy model. Methods XTreoTM matrices were formulated to consistently elute MF for up to 6 months. Matrices were surgically placed bilaterally into the maxillary sinuses of New Zealand White (NZW) rabbits. Tissue and plasma MF concentrations were measured to assess the in vivo drug delivery. The in vivo and in vitro drug release kinetics of the matrices were quantified and compared to those of rabbits receiving daily Nasonex® MF nasal sprays. Results XTreoTM matrices self-expanded upon deployment to conform to the irregular geometry of the maxillary sinus cavities in the NZW rabbits. Sustained release of MF was demonstrated in vitro and in vivo for 2 MF matrices of distinct release durations and an in vitro–in vivo correlation was established. Therapeutic levels of MF in local tissues were measured throughout the intended dosing durations. In contrast to the variable peaks and troughs of daily nasal sprays, sustained dosing via a single administration of MF matrices was confirmed by quantifiable plasma MF concentrations over the intended dosing duration. Conclusion The XTreoTM MF matrices provided targeted and efficient dosing to local sinus tissues that was superior to INCS. Sustained drug release was confirmed both in vitro and in vivo. The novel XTreoTM technology may provide precisely tuned, long-lasting drug delivery to sinus tissues with a single treatment.

scholarly journals Guar gum and hydroxy propyl methylcellulose compressed coated tablets for colonic drug delivery: in vitro and in vivo evaluation in healthy human volunteers

2011 ◽  
Vol 5 (2) ◽  
pp. 90-95 ◽  
Author(s):  
Fahima M. Hashem ◽  
Dalia S. Shaker ◽  
Mohamed Nasr ◽  
Ibrahim E. Saad ◽  
Reem Ragaey
Keyword(s):  
Drug Delivery ◽  
Guar Gum ◽  
Healthy Human ◽  
Colonic Drug Delivery ◽  
Human Volunteers

Preparation and In vivo Evaluation of Mucoadhesive Microspheres for Gastroretentive Delivery of Misoprostol

2017 ◽  
Vol 10 (2) ◽  
pp. 3676-3683
Author(s):  
Bhikshapathi D.V. R. N. ◽  
Ranjith Kumar K
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Gi Tract ◽  
In Vivo Evaluation ◽  
Upper Gi ◽  
Upper Gi Tract

The aim of the present investigation was to prepare and evaluate the Misoprostol mucoadhesive microspheres for gastroretentive drug delivery. Sodium alginate and sodium carboxy methyl cellulose were used as mucoadhesive polymers. Microsphere formulations were prepared using Ionotropic gelation technique. All the microspheres were characterized for particle size, scanning electron microscopy, FT-IR study, percentage yield, drug entrapment, stability studies and for in vitro release kinetics. Based on the results, the formulation M12 was selected as optimized formulation. In vitro drug release study of optimized formulation M12 showed 98.23% after 12 h in a controlled manner, which is essential for anti ulcer therapy. The marketed product shows the drug release of 95.23 within 1 h. The results of mucoadhesion study showed better retention of prepared microspheres (8) h in chic duodenal and jejunum regions of intestine. The results showed significant higher retention of mucoadhesive microspheres in upper GI tract. Pharmacokinetic study revealed that the bioavailability was found to be increased significantly when compared with marketed tablets. The drug release of Misoprostol optimized formulation M12 followed zero order, Higuchi and Korsmeyer-Peppas kinetics indicating diffusion controlled with non-Fickian (anomalous) transport thus it projected that delivered its active ingredient by coupled diffusion and erosion. Overall, the result indicated prolonged delivery with improved bioavailability of Misoprostol from mucoadhesive microspheres due to higher retention in the upper GI tract.

A Study of Mucoadhesive Bond Strength of Buccoadhesive Compacts for Systemic Drug Delivery: In-vitro/ In-vivo correlation

2001 ◽  
Vol 69 (2) ◽  
pp. 123-141
Author(s):  
D. Kumar ◽  
J. Balasubramaniam ◽  
J. Pandit
Keyword(s):  
Drug Delivery ◽  
Bond Strength ◽  
Buccal Mucosa ◽  
Healthy Human ◽  
Human Volunteers ◽  
Intestine Mucosa ◽  
Systemic Drug Delivery ◽  
Systemic Drug

Compacts prepared from binary combinations of Carbopol® 934 P (CP), Polycarbophil (Noveon® AA1, PC) and Hydroxy propyl cellulose (Klucel®, HPC) and coated on all but one flat surface with Poly Methyl Methacrylate - PMMA (chloroformic solution) were evaluated for mucoadhesive bond strength on a modified mucoadhesive bond strength apparatus using rabbit stomach mucosa (SM) and small intestine mucosa (SIM). In -vitro mucoadhesion tests indicated that the detachment force increased linearly with concentration of CP/PC in the compacts. Mucoadhesion of the compacts with SIM were higher when compared to SM. The compacts with higher proportions of CPIPC showed longer buccoadhesion time (time the compact remained in contact with the buccal mucosa) than HPC alone in humans. In-vivo buccoadhesevity of the coated compacts was studied in healthy human volunteers. An index was used to study the redness and ulceration of the contact buccal mucosa. Compacts with higher proportions of CP/PC showed longer buccoadhesion time than HPC alone. Significant correlation coefficient (r) values (P<0.01) were obtained between in-vitro fracture strength of the compacts and in-vivo buccoadhesion time. Hence, the in-vitro mucoadhesive model developed by us provides useful information on the residence time of the compact for systemic drug delivery in the oral cavity, and compacts containing less than 50% of CP/PC were safer to use in humans.

scholarly journals Development of a biodegradable antifibrotic local drug delivery system for glaucoma microstents

2018 ◽  
Vol 38 (4) ◽  
Author(s):  
Thomas Stahnke ◽  
Stefan Siewert ◽  
Thomas Reske ◽  
Wolfram Schmidt ◽  
Klaus-Peter Schmitz ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Kinetics ◽  
Caffeic Acid Phenethyl Ester ◽  
Local Drug Delivery ◽  
Fat Depots ◽  
Fat Depot ◽  
Local Drug Delivery System

To prevent implant failure due to fibrosis is a major objective in glaucoma research. The present study investigated the antifibrotic effects of paclitaxel (PTX), caffeic acid phenethyl ester (CAPE), and pirfenidone (PFD) coated microstent test specimens in a rat model. Test specimens based on a biodegradable blend of poly(4-hydroxybutyrate) biopolymer and atactic poly(3-hydroxybutyrate) (at.P(3HB)) were manufactured, equipped with local drug delivery (LDD) coatings, and implanted in the subcutaneous white fat depot. Postoperatively, test specimens were explanted and analyzed for residual drug content. Fat depots including the test specimens were histologically analyzed. In vitro drug release studies revealed an initial burst for LDD devices. In vivo, slow drug release of PTX was found, whereas it already completed 1 week postoperatively for CAPE and PFD LDD devices. Histological examinations revealed a massive cell infiltration in the periphery of the test specimens. Compact fibrotic capsules around the LDD devices were detectable at 4–36 weeks and least pronounced around PFD-coated specimens. Capsules stained positive for extracellular matrix (ECM) components. The presented model offers possibilities to investigate release kinetics and the antifibrotic potential of drugs in vivo as well as the identification of more effective agents for a novel generation of drug-eluting glaucoma microstents.

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