scholarly journals Design and In Vitro Evaluation of Chrono Modulated Theophylline Tablets

1970 ◽  
Vol 1 (1) ◽  
pp. 25-28
Author(s):  
B Vijaya Kumar ◽  
B Nagaraj ◽  
B Agaiah ◽  
D Rambhau
Keyword(s):  
Drug Delivery ◽  
Key Words ◽  
Delivery System ◽  
Research Work ◽  
Lag Phase ◽  
Enteric Polymer ◽  
Key Words Theophylline ◽  
Model Drug ◽  
Core Tablet

The objective of this research work was to prepare a chrono modulated delivery system to meet chronopharmacological needs of asthma. In this study theophylline was selected as a model drug. To meet this objective we considered an initial lag phase of release for 3-5 hrs and later a rapid (surge) release phase. To achieve surge release a rapidly releasing core tablet of theophylline was developed by admixing theophylline with effervescent granules and super disintegrants. The lag phase in release was achieved by coating the EV core tablets with release retarding polymer EUDRAGIT RS-100 containing HPMC, further over coated with enteric polymer CAP. The results indicate that a rapidly releasing EV tablet of theophylline cab be developed which when coated with the polymers a lag phase of 2 hrs was achievable followed by a surge release. Key Words: Theophylline, Chrono Modulated Drug Delivery, Asthma. doi:10.3329/sjps.v1i1.1782 S. J. Pharm. Sci. 1(1&2): 25-28

scholarly journals A Solid Ultra Fine Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) of Deferasirox for Improved Solubility: Optimization, Characterization, and In Vitro Cytotoxicity Studies

2020 ◽  
Vol 13 (8) ◽  
pp. 162 ◽  
Author(s):  
Alaa Alghananim ◽  
Yıldız Özalp ◽  
Burcu Mesut ◽  
Nedime Serakinci ◽  
Yıldız Özsoy ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cell Viability ◽  
Drug Delivery System ◽  
Delivery System ◽  
Research Work ◽  
Myelogenous Leukemia ◽  
Leukemia Cell Line ◽  
Dissolution Behavior ◽  
Cytotoxicity Studies

The research work was designed to develop a solid self-nanoemulsifying drug delivery system (S-SNEDDS) of deferasirox (DFX). According to the solubility studies of DFX in different components, Peceol, Kolliphor EL, and Transcutol were selected as excipients. Pseudo-ternary phase diagrams were constructed, and then SNEDDS formation assessment studies and solubility of DFX in selected SNEDDSs formulations were performed. DFX loaded SNEDDS were prepared and characterized. The optimum DFX-SNEDDS formulations were developed. The relative safety of the optimized SNEDDS formulation was examined in a human immortalized myelogenous leukemia cell line, K562 cells, using the MTT cell viability test. Cytotoxicity studies revealed more cell viability (71.44%) of DFX loaded SNEDDS compared to pure DFX (3.99%) at 40 μM. The selected DFX-SNEDDS formulation was converted into S-SNEDDS by adsorbing into porous carriers, in order to study its dissolution behavior. The in vitro drug release studies indicated that DFX release (Q5%) from S-SNEDDS solidified with Neusilin UFL2 was significantly higher (93.6 ± 0.7% within 5 min) compared with the marketed product (81.65 ± 2.10%). The overall results indicated that the S-SNEDDS formulation of DFX could have the potential to enhance the solubility of DFX, which would in turn have the potential to improve its oral bioavailability as a safe novel delivery system.

scholarly journals Folic Acid-Functionalized Black Phosphorus Quantum Dots for Targeted Chemo-Photothermal Combination Cancer Therapy

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 242 ◽  
Author(s):  
Miaomiao Luo ◽  
Wei Cheng ◽  
Xiaowei Zeng ◽  
Lin Mei ◽  
Gan Liu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Quantum Dots ◽  
Folic Acid ◽  
Drug Delivery System ◽  
Delivery System ◽  
Black Phosphorus ◽  
Model Drug ◽  
Black Phosphorus Quantum Dots

Due to the inherent limitations, single chemo or photothermal therapies (PTT) are always inefficient. The combination of chemotherapy and PTT for the treatment of cancers has attracted a great interest during the past few years. As a photothermal agent, black phosphorus quantum dots (BPQDs) possess an excellent extinction coefficient, high photothermal conversion efficacy, and good biocompatibility. Herein, we developed a photo- and pH-sensitive nanoparticle based on BPQDs for targeted chemo-photothermal therapy. Doxorubicin (DOX) was employed as a model drug. This nanosystem displayed outstanding photothermal performance both in vitro and in vivo. Folic acid conjugation onto the surface endowed this system an excellent tumor-targeting effect, which was demonstrated by the cellular targeting assay. The BPQDs-based drug delivery system exhibited pH- and photo-responsive release properties, which could reduce the potential damage to normal cells. The in vitro cell viability study showed a synergistic effect in suppressing cancer cell proliferation. Therefore, this BPQDs-based drug delivery system has substantial potential for future clinical applications.

Electrospun MWCNTs/Poly(lactic-co-glycolic acid) Composite Nanofibrous Drug Delivery System

2012 ◽  
Vol 424-425 ◽  
pp. 1220-1223 ◽  
Author(s):  
Rui Ling Qi ◽  
Hui Juan Liu
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Carriers ◽  
Mouse Fibroblast ◽  
Burst Release ◽  
Vis Spectroscopy ◽  
Multi Walled Carbon Nanotubes ◽  
Model Drug

In this study, nanotubular materials multi-walled carbon nanotubes (MWCNTs) were used to encapsulate a model drug, doxorubicine hydrochloride (DOX). Then, the drug-loaded nanotubes (DOX/CNTs) with an optimized drug encapsulation percentage were mixed with poly (lactide-co-glycolide) (PLGA) polymer solution for subsequent electrospinning to form drug-loaded composite nanofibrous mats. The morphology was characterized using scanning electron microscopy (SEM). The proliferation of mouse fibroblast cells cultured on both PLGA and CNTs-doped PLGA fibrous scaffolds were compared through 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyl tetrazolium bromide (MTT) assay of cell viability and SEM observation of cell morphology. In vitro drug release behavior was examined using UV-vis spectroscopy. We show that the incorporation of CNTs and DOX/CNTs within the nanofibrous mats does not significantly change the morphology of the mats. In addition, our results indicate that this double-container drug delivery system (both PLGA polymer and CNTs are drug carriers) is beneficial to avoid the burst release of the drug. The drug loaded elctrospinning composite nanofibrous mats developed in this study may find various applications in tissues engineering and pharmaceutical sciences.

scholarly journals A two pulse drug delivery system for amoxicillin: An attempt to counter the scourge of bacterial resistance against antibiotics

2011 ◽  
Vol 61 (3) ◽  
pp. 313-322 ◽  
Author(s):  
Habban Akhter ◽  
Nitin Saigal ◽  
Sanjula Baboota ◽  
Shah Faisal ◽  
Javed Ali
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Microcrystalline Cellulose ◽  
Bacterial Resistance ◽  
Lag Time ◽  
Pore Former ◽  
The Core ◽  
Core Tablet

A two pulse drug delivery system for amoxicillin: An attempt to counter the scourge of bacterial resistance against antibiotics Bearing in mind the present scenario of the increasing biological tolerance of bacteria against antibiotics, a time controlled two pulse dosage form of amoxicillin was developed. The compression coating inlay tablet approach was used to deliver the drug in two pulses to different parts of the GIT after a well defined lag time between the two releases. This was made possible by formulating a core containing one of the two drug fractions (intended to be delivered as the second pulse), which was spray coated with a suspension of ethyl cellulose and a hydrophilic but water insoluble agent as a pore former (microcrystalline cellulose). Coating of up to 5 % (m/m) was applied over the core tablet, giving a corresponding lag of 3, 5, 7 and 12 h. Increasing the level of coating led to retardation of the water uptake capacity of the core, leading to prolongation of the lag time. Microcrystalline cellulose was used as a hydrophilic but water insoluble porosity modifier in the barrier layer, varying the concentration of which had a significant effect on shortening or prolongation of the lag time. This coated system was further partially compression coated with the remaining drug fraction (to be released as the first immediate release pulse) with a disintegrant, giving a final tablet. The core tablet and the final two pulse inlay tablet were further investigated for their in vitro performance.

scholarly journals FORMULATION AND EVALUATION OF PULSATILE DRUG DELIVERY SYSTEM OF SALBUTAMOL SULFATE FOR THE CHRONOTHERAPY OF ASTHMA

2018 ◽  
Vol 11 (9) ◽  
pp. 305
Author(s):  
Chiranjibi Adhikari ◽  
Gururaj S Kulkarni ◽  
Shivakumar Swamy
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Release Profile ◽  
Salbutamol Sulfate ◽  
Pulsatile Drug Delivery ◽  
Core Tablet

Objective: The main objective of the present study was to design and evaluate a time-controlled single unit oral pulsatile drug delivery system containing salbutamol sulfate for the prevention of nocturnal asthma attacks.Methods: Drug containing core tablets (C1-C10) with different composition of superdisintegrants such as sodium starch glycolate, croscarmellose sodium, and crospovidone were prepared by direct compression technique. The fast disintegrating core tablet formulation was selected, and press-coated tablets (P1-P11) were prepared with different compositions of hydrophobic and hydrophilic polymers: Ethylcellulose-20 (EC-20), hydroxypropyl methylcellulose K4M, and low substituted hydroxypropyl cellulose (L-HPC LH11). The coating polymers were selected and quantified based on in vitro lag time and drug release profile in simulated gastric and intestinal fluids.Results: Formulation C10 with 7.5% crospovidone showed least disintegrating time, i.e., 0.31 min and was selected as the best immediate release core tablet. The press-coated tablet formulation P11 having 360 mg barrier layer of EC-20 and L-HPC LH11 in ratio 14:1 over the core tablet C10 showed rapid and complete drug release nearly after 6 h lag time. Accelerated stability studies of the optimized formulation P11 indicated no significant difference in release profile after a period of 6 months.Conclusion: The in vitro dissolution study showed that lag time before drug release was highly affected by the coating level and nature of coating polymer used. Time-controlled pulsatile release tablets can be prepared using press-coating techniques.

scholarly journals Development and Evaluation of Gastro-retentive Floating Tablet of Rilpivirine Hydrochloride for the Treatment of HIV

2020 ◽  
Vol 10 (3-s) ◽  
pp. 43-46
Author(s):  
Dipali Trivedi ◽  
Arti Majumdar ◽  
Neelesh Malviya
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Residence Time ◽  
Delivery System ◽  
Research Work ◽  
Water Soluble ◽  
Gastric Residence Time ◽  
Floating Drug Delivery ◽  
Gastro Retentive

Besides enormous improvements in drug delivery, oral route has been highly and effectively utilized route of administration. Floating drug delivery that is also known to be low density system is advancement in the class of gastro-retentive drug delivery system. In the present research work, floating drug delivery of Rilpivirine hydrochloride was developed by overcoming various limitations and troubles associated with the drug including poor absorption in intestinal pH and degradation when comes in contact with higher pH environment. [2] Prepared formulations were evaluated for various parameters like friability, hardness, thickness, drug content analysis, floating properties and in-vitro drug release study. Based on the evaluation, concluded that floating drug delivery system is a non-toxic as well as cost-effective technique for the rationale of enhancing bioavailability and absorption of poorly water soluble drugs. The improvement in gastric residence time is a clear sign. It can be able to use in the future for more acidic soluble drugs to enhance solubility and absorption. Keywords: Floating drug delivery, gastric residence time, Rilpivirine, effervescent, NNRTI.

NO-Responsive vesicles as a drug delivery system

2017 ◽  
Vol 53 (25) ◽  
pp. 3535-3538 ◽  
Author(s):  
Zhi-Heng Li ◽  
Zheng-Li Tan ◽  
Ai-Xiang Ding ◽  
Bing Gong ◽  
Zhong-Lin Lu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Aqueous Solution ◽  
Drug Delivery System ◽  
Delivery System ◽  
Living Cells ◽  
System P ◽  
Model Drug ◽  
And Control

A NO-response amphiphile was successfully formed into vesicles in aqueous solution, which could encapsulate and control the release of carboxyfluorescein (CF) as a model drug in vitro and in living cells.

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.

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