scholarly journals A Novel Multilayered Multidisk Oral Tablet for Chronotherapeutic Drug Delivery

2013 ◽  
Vol 2013 ◽  
pp. 1-16 ◽  
Author(s):  
Zaheeda Khan ◽  
Yahya E. Choonara ◽  
Pradeep Kumar ◽  
Lisa C. du Toit ◽  
Valence M. K. Ndesendo ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Aqueous Dispersion ◽  
Lag Phase ◽  
Oral Tablet ◽  
Barrier Layers ◽  
Swelling Studies ◽  
Diltiazem Hcl ◽  
Drug Free ◽  
Delayed Drug Release

A Multilayered Multidisk Tablet (MLMDT) comprising two drug-loaded disks enveloped by three drug-free barrier layers was developed for use in chronotherapeutic disorders, employing two model drugs, theophylline and diltiazem HCl. The MLMDT was designed to achieve two pulses of drug release separated by a lag phase. The polymer disk comprised hydroxyethylcellulose (HEC) and ethylcellulose (EC) granulated using an aqueous dispersion of EC. The polymeric barrier layers constituted a combination of pectin/Avicel (PBL) (1st barrier layer) and hydroxypropylmethylcellulose (HPMC) (HBL1 and HBL2) as the 2nd and 3rd barrier layers, respectively. Sodium bicarbonate was incorporated into the diltiazem-containing formulation for delayed drug release. Erosion and swelling studies confirmed the manner in which the drug was released with theophylline formulations exhibiting a maximum swelling of 97% and diltiazem containing formulations with a maximum swelling of 119%. FTIR spectra displayed no interactions between drugs and polymers. Molecular mechanics simulations were undertaken to predict the possible orientation of the polymer morphologies most likely affecting the MLMDT performance. The MLMDT provided two pulses of drug release, separated by a lag phase, and additionally it displayed desirable friability, hardness, and uniformity of mass indicating a stable formulation that may be a desirable candidate for chronotherapeutic drug delivery.

Development and Evaluation of Floating Pulsatile Drug Delivery System Using Meloxicam

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
ShirishaG. Suddala ◽  
S. K. Sahoo ◽  
M. R. Yamsani
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Oral Dosage ◽  
Lag Phase ◽  
Pulsatile Drug Delivery

Objective: The objective of this research work was to develop and evaluate the floating– pulsatile drug delivery system (FPDDS) of meloxicam intended for Chrono pharmacotherapy of rheumatoid arthritis. Methods: The system consisting of drug containing core, coated with hydrophilic erodible polymer, which is responsible for a lag phase for pulsatile release, top cover buoyant layer was prepared with HPMC K4M and sodium bicarbonate, provides buoyancy to increase retention of the oral dosage form in the stomach. Meloxicam is a COX-2 inhibitor used to treat joint diseases such as osteoarthritis and rheumatoid arthritis. For rheumatoid arthritis Chrono pharmacotherapy has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Result and discussion: The prepared tablets were characterized and found to exhibit satisfactory physico-chemical characteristics. Hence, the main objective of present work is to formulate FPDDS of meloxicam in order to achieve drug release after pre-determined lag phase. Developed formulations were evaluated for in vitro drug release studies, water uptake and erosion studies, floating behaviour and in vivo radiology studies. Results showed that a certain lag time before drug release which was due to the erosion of the hydrophilic erodible polymer. The lag time clearly depends on the type and amount of hydrophilic polymer which was applied on the inner cores. Floating time and floating lag time was controlled by quantity and composition of buoyant layer. In vivo radiology studies point out the capability of the system of longer residence time of the tablets in the gastric region and releasing the drug after a programmed lag time. Conclusion: The optimized formulation of the developed system provided a lag phase while showing the gastroretension followed by pulsatile drug release that would be beneficial for chronotherapy of rheumatoid arthritis and osteoarthritis.

scholarly journals Novel Floating Pulsatile Approach for Chronotherapeutic Release of Indomethacin

1970 ◽  
Vol 6 (1) ◽  
pp. 37-41
Author(s):  
Shaji Jessy ◽  
Patole Vishal
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Delivery ◽  
Small Intestine ◽  
Drug Release ◽  
Basic Medium ◽  
Lag Phase ◽  
Burst Release ◽  
Distal Small Intestine ◽  
Pulsatile Drug Delivery ◽  
Time Specific

The main objective of the present study was to develop a multiple-unit, floating-pulsatile drug delivery system for obtaining no drug release during floating and in the proximal small intestine followed by pulsed, rapid drug release in distal small intestine to achieve chronotherapeutic release of indomethacin. The system developed consists of drug containing core pellets prepared by extrusion-spheronization process, which were coated with an inner pH-dependent layer of Eudragit S100 and outer effervescent layer of sodium bicarbonate and HPMC K100M. Pellets showed instantaneous floating with no drug release in acidic medium followed by pulsed drug release in basic medium. Concentration of HPMC K100M and layering level of effervescent agent significantly affected performance of pellets. The system showed excellent lag phase followed by burst release in the distal small intestine which gives site and time specific delivery of indomethacin acting as per chronotherapy of rheumatoid arthritis. Key words: Floating-pulsatile drug delivery, Chronotherapeutic release, Indomethacin, Pellets, Rheumatoid arthritis. Dhaka Univ. J. Pharm. Sci. 6(1): 37-41, 2007 (June) The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

Nano Sponges

2019 ◽  
Vol 12 (6) ◽  
pp. 4687-4693
Author(s):  
Amarjit Salunke Salunke ◽  
Neeraj Upamanyu ◽  
Alka Singh ◽  
Ashish Jaiswal
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Drug Release ◽  
Recent Work ◽  
Delivery System ◽  
Therapeutic Index ◽  
Free Carriers ◽  
The Us ◽  
Work Done ◽  
Drug Free

The convenient and recent drug delivery system always likely to have some ideal and unique characters, particularly for safety, desired actions, accurate delivery, enrich with a therapeutic index with minimal adverse occurrence. In this regard, Nano sponges serve as a recent advance new drug delivery. Many researchers are attracted and concerned on Nano sponges presently. The present twofold objective of the review clarifies why Nano sponges are recent and advanced delivery system along with challenges related to solubility, stability and controlled release of Nano sponge and proven techniques to overcome. Since the nano-sized drug free carriers are recently formulated and suggested for drug delivery, which can be loaded with the numerous drugs, hence dealing with an appropriate technique for drug release is the need of the present time. This article states the most convenient method for drug release, and at concluding part gives awareness on recent work done and result obtained on Nano sponge worldwide along with the unique summary on the US granted patents for Nano sponges. Thus, a complete scenario on recent work, methods for evaluations, unique and multiple characters of Nano sponge has been discussed and summarized.

scholarly journals Optimization Studies on Compression Coated Floating-Pulsatile Drug Delivery of Bisoprolol

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Swati C. Jagdale ◽  
Nilesh A. Bari ◽  
Bhanudas S. Kuchekar ◽  
Aniruddha R. Chabukswar
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Active Ingredient ◽  
Dosage Form ◽  
Release Kinetics ◽  
Lag Phase ◽  
Burst Release ◽  
Release Formulation ◽  
Pulsatile Drug Delivery ◽  
Core Tablet

The purpose of the present work was to design and optimize compression coated floating pulsatile drug delivery systems of bisoprolol. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. The prepared system consisted of two parts: a core tablet containing the active ingredient and an erodible outer shell with gas generating agent. The rapid release core tablet (RRCT) was prepared by using superdisintegrants with active ingredient. Press coating of optimized RRCT was done by polymer. A 32full factorial design was used for optimization. The amount of Polyox WSR205 and Polyox WSR N12K was selected as independent variables. Lag period, drug release, and swelling index were selected as dependent variables. Floating pulsatile release formulation (FPRT) F13 at level 0 (55 mg) for Polyox WSR205 and level +1 (65 mg) for Polyox WSR N12K showed lag time of 4 h with >90% drug release. The data were statistically analyzed using ANOVA, andP<0.05was statistically significant. Release kinetics of the optimized formulation best fitted the zero order model.In vivostudy confirms burst effect at 4 h in indicating the optimization of the dosage form.

scholarly journals DESIGN AND DEVELOPMENT OF FLOATING PULSATILE DRUG DELIVERY OF LOSARTAN POTASSIUM

2020 ◽  
pp. 218-227
Author(s):  
ANIL KUMAR J. SHINDE ◽  
NIDHI S. PATIL ◽  
TRUPTI S. JADHAV ◽  
HARINATH N. MORE
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Lag Time ◽  
Losartan Potassium ◽  
In Vitro Dissolution ◽  
Lag Phase ◽  
Burst Release ◽  
Distal Small Intestine ◽  
Pulsatile Drug Delivery

Objective: The objective of the present investigation was to the development of floating pulsatile drug delivery system of Losartan potassium (LP) tablets for obtaining no drug release during floating followed by pulsed, rapid drug release to achieve chronotherapeutic release. In hypertension, the risk of getting heart attacks early in the morning is high and therefore, there was need to develop drug delivery, which will release drugs at morning hours and provide efficacious therapy. LP is a short biological half-life (1.5-2.5h) and readily absorbed from the stomach and upper gastrointestinal tract. Methods: Tablet formulation was prepared by press coating of rapid release core tablets and core tablets were further top coated with a buoyant layer of HPMC K4M and sodium bicarbonate. Various grades of HPMC polymer (E5/E15/E50) were used for the pulsatile coating layer. The developed formulations were characterized for physical characteristics, floating lag time, floating time, release lag time, drug content, swelling index, in vitro dissolution studies, DSC and XRD. Results: The FTIR and DSC studies predicted that there was no chemical interaction between drug and excipients. The core tablet coated with HPMC E50 showed a high swelling index and release the drug 97.60±1.2% at 6h. Buoyant layer with 80 mg HPMC K4M and 25 mg sodium bicarbonate gave satisfactory floating lag time. Conclusion: The system showed an excellent lag phase followed by burst release in the distal small intestine, which gives site and time-specific delivery of LP acting as per chronotherapy for treatment of hypertension.

The Improvement of Paclitaxel Cytotoxicity using Nanocellulose based Nature Resources

2019 ◽  
Vol 1 (1) ◽  
pp. 7
Author(s):  
R Nahrowi ◽  
A Setiawan ◽  
Noviany Noviany ◽  
I Sukmana ◽  
S D Yuwono
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Natural Resources ◽  
Cell Viability ◽  
Cancer Cells ◽  
Drug Delivery System ◽  
Target Cell ◽  
Mitotic Cycle ◽  
Potential Sources ◽  
Local Accumulation

Paclitaxel is one of the cancer drugs that often used. These drug kills cancer cells byinhibiting mitotic cycle. The efficiency of paclitaxel is increased by the use ofnanomaterials as a carrier of paclitaxel. Nanomaterials can enhance encapsulationefficiency, improve the drug release to the target cell following nanomaterialdegradation, and improve local accumulation of drug in the cell through endocytosisreceptor. Nanomaterial that often used forencapsulation of paclitaxel is a polymerderived from natural resources such as cellulose. The advantages of cellulose as acarrier of paclitaxel are nontoxic, biodegradable, and very abundant from varioussources. One of the potential sources of cellulose for drug delivery system is cassavabaggase.Keywords: Paclitaxel, encapsulation, cell viability, nanocellulose

Acyclovir Loaded Solid Lipid Nanoparticle Based Cream: A Novel Drug Delivery System

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
EL- Assal I. A. ◽  
Retnowati .
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Antiviral Agent ◽  
Study Drug ◽  
Particle Size Analysis ◽  
Stability Study ◽  
Size Analysis ◽  
Solid Lipid ◽  
Dermal Delivery

Objective of the present investigation was enthused by the possibility to develop solid lipid nanoparticles (SLNs) of hydrophilic drug acyclovir. Also study vitro and vivo drug delivery. Methods: Drug loaded SLNs (ACV-SLNs) were prepared by high pressure homogenization of aqueous surfactant solutions containing the drug-loaded lipids in the melted or in the solid state with formula optimization study (Different lipid concentration, drug loaded, homogenization / stirring speed and compritol 888ATO: drug ratio). ACV - SLN incorporated in cream base. The pH was evaluated and rheological study. Drug release was evaluated and compared with simple cream- drug, ACV – SLN with compritol 888ATO and marketed cream. The potential of SLN as the carrier for dermal delivery was studied. Results: Particle size analysis of SLNs prove small, smooth, spherical shape particle ranged from 150 to 200 nm for unloaded and from 330 to 444 nm for ACV loaded particles. The EE% for optimal formula is 72% with suitable pH for skin application. Rheological behavior is shear thinning and thixotropic. Release study proved controlled drug release for SLNs especially in formula containing compritol88 ATO. Stability study emphasized an insignificant change in SLNs properties over 6 month. In-vivo study showed significantly higher accumulation of ACV in stratum corneum, dermal layer, and receptor compartment compared with blank skin. Conclusion: AVC-loaded SLNs might be beneficial in controlling drug release, stable and improving dermal delivery of antiviral agent(s).

Formulation, Development and Characterization of Floating Beads of Diltiazem Hydrochloride

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Anamika Saxena Saxena ◽  
Santosh Kitawat ◽  
Kalpesh Gaur ◽  
Virendra Singh
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Entrapment Efficiency ◽  
Repeated Administration ◽  
Alginate Beads ◽  
Delivery Systems ◽  
Sem Analysis ◽  
Formulation Development

The main goal of any drug delivery system is to achieve desired concentration of the drug in blood or tissue, which is therapeutically effective and nontoxic for a prolonged period. Various attempts have been made to develop gastroretentive delivery systems such as high density system, swelling, floating system. The recent developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. Background of the research: Diltiazem HCL (DTZ), has short biological half life of 3-4 h, requires rather high frequency of administration. Due to repeated administration there may be chances of patient incompliance and toxicity problems. Objective: The objective of study was to develop sustained release alginate beads of DTZ for reduction in dosing frequency, high bioavailability and better patient compliance. Methodology: Five formulations prepared by using different drug to polymer ratios, were evaluated for relevant parameters and compared. Alginate beads were prepared by ionotropic external gelation technique using CaCl2 as cross linking agent. Prepared beads were evaluated for % yield, entrapment efficiency, swelling index in 0.1N HCL, drug release study and SEM analysis. In order to improve %EE and drug release, LMP and sunflower oil were used as copolymers along with sodium alginate.

Development of Solid Lipid Nanoparticles of Lamivudine for Brain Targeting

2009 ◽  
Vol 1 (1) ◽  
Author(s):  
Pravin Patil ◽  
Anil Sharma ◽  
Subhash Dadarwal ◽  
Vijay Sharma
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Rotation Speed ◽  
Lipid Nanoparticles ◽  
Brain Targeting ◽  
Brain Penetration ◽  
Solid Lipid ◽  
Diffusion Technique

The objective of present investigation was to enhance brain penetration of Lamivudine, one of the most widely used drugs for the treatment of AIDS. This was achieved through incorporating the drug into solid lipid nanoparticles (SLN) prepared by using emulsion solvent diffusion technique. The formulations were characterized for surface morphology, size and size distribution, percent drug entrapment and drug release. The optimum rotation speed, resulting into better drug entrapment and percent yield, was in the range of 1000-1250 r/min. In vitro cumulative % drug release from optimized SLN formulation was found 40-50 % in PBS (pH-7.4) and SGF (pH-1.2) respectively for 10 h. After 24 h more than 65 % of the drug was released from all formulations in both mediums meeting the requirement for drug delivery for prolong period of time.

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