scholarly journals A New Model for Zero-Order Drug Release I. Hydrophobic Drug Release from Hydrophilic Polymeric Matrices

1991 ◽  
Vol 23 (9) ◽  
pp. 1111-1121 ◽  
Author(s):  
Ryo Yoshida ◽  
Kiyotaka Sakai ◽  
Teruo Okano ◽  
Yasuhisa Sakurai
Keyword(s):  
Drug Release ◽  
Zero Order ◽  
Hydrophobic Drug ◽  
Polymeric Matrices ◽  
New Model

A new model of resorbable device degradation and drug release - part I: zero order model

2008 ◽  
Vol 57 (7) ◽  
pp. 912-920 ◽  
Author(s):  
Paolo Arosio ◽  
Valentina Busini ◽  
Giuseppe Perale ◽  
Davide Moscatelli ◽  
Maurizio Masi
Keyword(s):  
Drug Release ◽  
Zero Order ◽  
Order Model ◽  
New Model

Formulation and Evaluation of Nelfinavir Extended Release Trilayer Matrix Tablets by Design of Experiment

2018 ◽  
Vol 11 (5) ◽  
pp. 4259-4268
Author(s):  
Nirmala Rangu ◽  
Gande Suresh
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Magnesium Stearate ◽  
Zero Order ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Crystalline Cellulose ◽  
Dissolution Profile ◽  
Release Formulation

The present study was aimed to develop once-daily controlled release trilayer matrix tablets of nelfinavir to achieve zero-order drug release for sustained plasma concentration. Nelfinavir trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC), PVP (Polyvinyl Pyrrolidine) K-30 and MCC (Micro Crystalline Cellulose). Barrier layers were prepared with Polyox WSR-303, Xanthan gum, microcrystalline cellulose and magnesium stearate. Based on the evaluation parameters, drug dissolution profile and release drug kinetics DF8 were found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (DF8) was described by the zero-order and best fitted to Higuchi model. FT-IR studies confirmed that there were no chemical interactions between drug and excipients used in the formulation. These results indicate that the approach used could lead to a successful development of a controlled release formulation of nelfinavir in the management of AIDS.

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.  

Formulation Development and Characterization of controlled release core in cup matrix tablets of venlafaxine HCl

2020 ◽  
Vol 15 ◽  
Author(s):  
Balaji Maddiboyina ◽  
Vikas Jhawat ◽  
Gandhi Sivaraman ◽  
Om Prakash Sunnapu ◽  
Ramya Krishna Nakkala ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Rate ◽  
Zero Order ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Crystalline Cellulose ◽  
Hydrophobic Polymers

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.

Drug release from viscoelastic polymeric matrices - a stable and supraconvergent FDM

2021 ◽  
Vol 99 ◽  
pp. 257-269
Author(s):  
J.S. Borges ◽  
J.A. Ferreira ◽  
G. Romanazzi ◽  
E. Abreu
Keyword(s):  
Drug Release ◽  
Polymeric Matrices

Fabrication and Release Kinetics of Liposomes Containing Leuprolide Acetate

2021 ◽  
Vol 7 (1) ◽  
pp. 35-38
Author(s):  
Sudipta Das ◽  
Arnab Samanta ◽  
Koushik Bankura ◽  
Debatri Roy ◽  
Amit Nayak
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Zero Order ◽  
Leuprolide Acetate ◽  
Lipid Film ◽  
In Vitro Drug Release ◽  
Liposomal Formulations ◽  
Kinetics Of

The present work is focused on the preparation and in vitro release kinetics of liposomal formulation of Leuprolide Acetate. In this work, “Thin Lipid Film Hydration Method” was used for preparation of Leuprolide Acetate loaded liposomes. Prepared liposomal formulations of Leuprolide acetate was evaluated by drug entrapment study, in-vitro drug release kinetics and stability studies. The percentage drug entrapment of Leuprolide acetate for F1 and F2 formulations were found to be 78.14 ± 0.67 and 66.70 ± 0.81% respectively. In-vitro drug release study of liposomal formulations had shown zero order release pattern. Regression co-efficient (R2) value of Zero order kinetics for F1 and F2 formulations were 0.9912 and 0.9676 respectively. After storing formulations for 1 month, stability testing was done at 40C.It was found that all batches were stable. These liposomal formulations of Leuprolide acetate can be formulated for parenteral application to treat prostate cancer and in women, to treat symptoms of endometriosis (overgrowth of uterine lining outside of the uterus) or uterine fibroids.

In silicomechanistic disposition andin vivoevaluation of zero-order drug release from a novel triple-layered tablet matrix

2014 ◽  
Vol 12 (5) ◽  
pp. 693-713 ◽  
Author(s):  
Kovanya Moodley ◽  
Yahya E Choonara ◽  
Pradeep Kumar ◽  
Lisa C du Toit ◽  
Viness Pillay
Keyword(s):  
Drug Release ◽  
Zero Order ◽  
Tablet Matrix

scholarly journals Different Approaches to the Synthesis and Applications of Biomedical and Pharmaceutical Smart Biomaterials

2021 ◽  
Author(s):  
Mohamed Mahmoud Khattab
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Degradation Rate ◽  
Zero Order ◽  
Porous Scaffolds ◽  
Bulk Properties ◽  
Cellulose Nanowhisker ◽  
Order Release ◽  
Hemp Hurd

In this study, two strategies were used to functionalize cellulose nanowhiskers. Firstly, by grafting its surface with β-cyclodextrin (βCD) for developing drug-nanocarrier. Secondly, by conjugating short polymer segments to its surface for reinforcing Poly(Ɛ-Caprolactone) (PCL), in order to develop nanocomposites with promoted properties suitable for regenerative medicine. In addition, the production and recovery of biodegradable bioplastics poly(3-hydroxybutyrate) (P(3HB)) from agro-industrial residues of hemp hurd biomass was also examined. In the first part, a drug-nanocarrier system based on βCD-grafted bacterial cellulose nanowhisker (BCNC-g-βCD) was developed as a prolonged drug release nanocarrier. Antibiotic Ciprofloxacin (CIP) and anticancer drugs; Doxorubicin (DOX) and Paclitaxel (PTX) were conjugated to BCNC-g-βCD as model drugs to form the drug-nanocarrier (BCNC-g-βCD-drug). Compared with un-grafted BCNC, the developed drug-nanocarrier showed significant increase in drug payloads from 495 ±4 to 810 ±7 µg/mg along with radical improvement in the drug release profiles. Initial burst releases was reduced significantly and prolonged and sustained release for (74.5–90%) of drug payload over 4–5.5 days were observed. In addition, an improved drug release performances were pragmatic in acidic pH of 6.4 that mimicked extracellular tumor cells. In vitro drug release data pointed to zero-order kinetic model with estimated zero-order release constants (K0) of 0.68, 0.74, and 0.79 µg drug/h (at pH 6.4, 37°C) for BCNC-g-βCD-CIP, BCNC-g-βCD-DOX and BCNC-g-βCD-PTX nanosystems, respectively. In the second part, the functionalized bacterial cellulose nanowhisker (BCNW-g-βCD-PCL2000) was synthesized. Reinforcing PCL matrix with 4 wt% of the functionalized nanowhisker resulted in bionanocomposite with promoted bulk properties. Compared to neat PCL, the obtained bionanocomposite showed 115% and 51% improvements in tensile strength and Young’s modulus, respectively; 20% increase in hydrophilicity; 7% increase in degradation rate; and 6% decrease in crystallinity. Gas foaming/combined particulate leaching technique is used to develop highly porous strutures having porosity of 86-95% and interconnected macropores with mean pore diameters of 250-420 µm. Porous scaffolds showed compression moduli values of 5.3-9.1 MPa in the range of cancellous bones. In the third part a dual-function PCL scaffold was fabricated. The envisioned drug-laden scaffold would provide adequate structural and mechanical supports for the newly regenerated tissues and simultaneously serve as localized drug delivery system. In this context, reinforced PCL with 4 wt% of BCNW-g-βCD-PCL2000 and 25 wt% of doxorubicin anticancer drug resulted in drugladen bionanocomposite of combined promoted bulk properties. Improvements of 165% and 107% in tensile strength and Young’s modulus, respectively; 31% in hydrophilicity; 10% in degradation rate; and 8°C increases in thermal stability. The obtained drug-laden porous scaffolds showed compressive moduli in the range of 7.2-12.3 MPa. In vitro drug releases fit the first-order release mechanism and occurred in a diffusion-controlled and sustained manner 60 days without obvious burst releases. The scaffolds will ultimately minimize systemic toxicities of drugs, lessen the number of dosing, and diminish the need for removal procedure. The forth study described prospective trials for greener production and extraction of the biodegradable bioplastics poly(3-hydroxybutyrate) P(3HB) from agro-industrial residues of hemp hurd biomass. Results showed that maximum hydrolysis yield of 72.4% was achieved by alkali pretreatment with 2% NaOH at 135°C for 60 min along with two-step enzymatic hydrolysis and ultrasonication. Total hydrolysate sugar concentration of 53.0 g/L was obtained. Under optimum conditions, total P(3HB) production of 13.4 g/L was achieved within 80 h of fermentation. Ultrasonic-assisted sodium dodecyl sulfate (SDS) has showed effectiveness as economic recovery method. It recovered bioplastics directly from the broth cell concentrate with P(3HB) content of 92%. Number average molecular weights (Mn) of recovered bioplastics were in the range of 150–270 kDa with polydispersity index (Mw/Mn) of 2.1–2.4.

scholarly journals Different Approaches to the Synthesis and Applications of Biomedical and Pharmaceutical Smart Biomaterials

2021 ◽  
Author(s):  
Mohamed Mahmoud Khattab
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Degradation Rate ◽  
Zero Order ◽  
Porous Scaffolds ◽  
Bulk Properties ◽  
Cellulose Nanowhisker ◽  
Order Release ◽  
Hemp Hurd

In this study, two strategies were used to functionalize cellulose nanowhiskers. Firstly, by grafting its surface with β-cyclodextrin (βCD) for developing drug-nanocarrier. Secondly, by conjugating short polymer segments to its surface for reinforcing Poly(Ɛ-Caprolactone) (PCL), in order to develop nanocomposites with promoted properties suitable for regenerative medicine. In addition, the production and recovery of biodegradable bioplastics poly(3-hydroxybutyrate) (P(3HB)) from agro-industrial residues of hemp hurd biomass was also examined. In the first part, a drug-nanocarrier system based on βCD-grafted bacterial cellulose nanowhisker (BCNC-g-βCD) was developed as a prolonged drug release nanocarrier. Antibiotic Ciprofloxacin (CIP) and anticancer drugs; Doxorubicin (DOX) and Paclitaxel (PTX) were conjugated to BCNC-g-βCD as model drugs to form the drug-nanocarrier (BCNC-g-βCD-drug). Compared with un-grafted BCNC, the developed drug-nanocarrier showed significant increase in drug payloads from 495 ±4 to 810 ±7 µg/mg along with radical improvement in the drug release profiles. Initial burst releases was reduced significantly and prolonged and sustained release for (74.5–90%) of drug payload over 4–5.5 days were observed. In addition, an improved drug release performances were pragmatic in acidic pH of 6.4 that mimicked extracellular tumor cells. In vitro drug release data pointed to zero-order kinetic model with estimated zero-order release constants (K0) of 0.68, 0.74, and 0.79 µg drug/h (at pH 6.4, 37°C) for BCNC-g-βCD-CIP, BCNC-g-βCD-DOX and BCNC-g-βCD-PTX nanosystems, respectively. In the second part, the functionalized bacterial cellulose nanowhisker (BCNW-g-βCD-PCL2000) was synthesized. Reinforcing PCL matrix with 4 wt% of the functionalized nanowhisker resulted in bionanocomposite with promoted bulk properties. Compared to neat PCL, the obtained bionanocomposite showed 115% and 51% improvements in tensile strength and Young’s modulus, respectively; 20% increase in hydrophilicity; 7% increase in degradation rate; and 6% decrease in crystallinity. Gas foaming/combined particulate leaching technique is used to develop highly porous strutures having porosity of 86-95% and interconnected macropores with mean pore diameters of 250-420 µm. Porous scaffolds showed compression moduli values of 5.3-9.1 MPa in the range of cancellous bones. In the third part a dual-function PCL scaffold was fabricated. The envisioned drug-laden scaffold would provide adequate structural and mechanical supports for the newly regenerated tissues and simultaneously serve as localized drug delivery system. In this context, reinforced PCL with 4 wt% of BCNW-g-βCD-PCL2000 and 25 wt% of doxorubicin anticancer drug resulted in drugladen bionanocomposite of combined promoted bulk properties. Improvements of 165% and 107% in tensile strength and Young’s modulus, respectively; 31% in hydrophilicity; 10% in degradation rate; and 8°C increases in thermal stability. The obtained drug-laden porous scaffolds showed compressive moduli in the range of 7.2-12.3 MPa. In vitro drug releases fit the first-order release mechanism and occurred in a diffusion-controlled and sustained manner 60 days without obvious burst releases. The scaffolds will ultimately minimize systemic toxicities of drugs, lessen the number of dosing, and diminish the need for removal procedure. The forth study described prospective trials for greener production and extraction of the biodegradable bioplastics poly(3-hydroxybutyrate) P(3HB) from agro-industrial residues of hemp hurd biomass. Results showed that maximum hydrolysis yield of 72.4% was achieved by alkali pretreatment with 2% NaOH at 135°C for 60 min along with two-step enzymatic hydrolysis and ultrasonication. Total hydrolysate sugar concentration of 53.0 g/L was obtained. Under optimum conditions, total P(3HB) production of 13.4 g/L was achieved within 80 h of fermentation. Ultrasonic-assisted sodium dodecyl sulfate (SDS) has showed effectiveness as economic recovery method. It recovered bioplastics directly from the broth cell concentrate with P(3HB) content of 92%. Number average molecular weights (Mn) of recovered bioplastics were in the range of 150–270 kDa with polydispersity index (Mw/Mn) of 2.1–2.4.

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