Chronomodulated Delivery of Pantoprazole for Nocturnal Hyperacidity

Author(s):  
Mahalakshmi P ◽  
Suriyaprakash T N K ◽  
S. Lakshmana Prabu

The objective of this work was to design and evaluate an oral site-specific, pulsatile drug delivery system containing Pantoprazole sodium which can be targeted to colon in a pH and time dependent manner, to modulate the drug level in synchrony with the circadian rhythm of nocturnal hyperacidity. Five different composition of Core tablets were prepared by direct compression technique. Based on the release studies of core tablets, nine different compositions of press coated tablets were prepared and analyzed. The press coated tablet further coated by using five different proportions of Eudragit RS PO for providing consistent, reproducible chronomodulated release profile. Formulation FPC3 is more suitable among the formulations to design pulsatile release formulations of pantoprazole sodium for 6 hours lag time. After this lag time burst release was observed which exhibited sigmodial release pattern and that was considered to be an ideal for the pulsatile drug delivery system. The chronomodulated drug delivery systems for pantoprazole sodium for the treatment of hyperacidity was successfully developed and the release of the drug was sharp and complete after the lag time which is necessary for any pulsatile drug delivery systems.   

Author(s):  
PASHAM SOWMYA ◽  
VENKATESH DP ◽  
SUJIT NAYEK

location at a particular time. Some of the conditions under which pulsatile drug delivery system is positive include duodenal ulcer, cardiovascular disease, arthritis, asthma, diabetes, neurological disorder, cancer, hypertension, and hypercholesterolemia. Pulsatile drug delivery systems are essentially time-controlled drug delivery systems in which the lag time is regulated independently of environmental factors such as pH, enzymes, gastrointestinal motility, etc. The theory justification for the use of pulsatile release is for drugs where a continuous release of drugs is not needed, i.e. a zero-order release. Drug administration in chronopharmacotherapy is coordinated with biological rhythms to achieve full therapeutic effect and minimize harm to the patient. This drug delivery system is designed to distribute drugs in accordance with body clock. The pulse must be designed in such a way as to achieve a total and rapid release after the lag time. Pulsatile drug delivery is therefore one device that provides strong promises of benefit to patients suffering from chronic conditions such as arthritis, asthma, hypertension by delivering medication at the right time, right place and in appropriate quantities. In recent pharmaceutical applications involving pulsatile delivery; multi-particulate dosage forms (e. g. pellets) over single-unit dosage forms are gaining more popularity. On the basis of methodologies, various pulsatile technologies have been developed, including ACCU-BREAKTM, AQUALON, CODAS ®, PRODAS ®, SODAS ®, MINITABS ®, DIFFUCAPS ®, OROS ® etc.


Clay Minerals ◽  
2018 ◽  
Vol 53 (1) ◽  
pp. 53-63 ◽  
Author(s):  
Faezeh Hosseini ◽  
Farzaneh Hosseini ◽  
Seyyed Mehdi Jafari ◽  
Azade Taheri

ABSTRACTLocal chemotherapy with biocompatible drug-delivery systems prolongs survival in patients. Due to the biocompatibility and high loading capacity, bentonite nanoclay is a good candidate for the fabrication of drug-delivery vehicles. In this study, doxorubicin-bentonite nanoclay complex (DOX-Bent complex) was prepared for the first time as a sustained-release drug-delivery system for intratumoural chemotherapy of melanoma. An efficient loading of DOX on 1 mg of bentonite nanoclay as high as 994.45 ± 4.9 µg was obtained at a 30:1 DOX:bentonite nanoclay mass ratio. The DOX-Bent complex showed a low initial burst release of DOX in the first 24 h of release, followed by a sustained-release pattern for 21 days. The cumulativein vitrorelease of DOX from the DOX-Bent complex at pHs 6.5 and 7.4 revealed that the DOX-Bent complex can distinguish between tumour and normal tissues and express specific drug release at the tumour site. The results of cytotoxicity experiments indicated that the release pattern of DOX can supply sufficient DOX to inhibit growth of the melanoma cancer cell with an IC50 of 0.29 ± 0.07 µg/mL. It is thus suggested that the DOX-Bent complex be introduced as a drug-delivery system for effective local cancer therapy.


Author(s):  
ShirishaG. Suddala ◽  
S. K. Sahoo ◽  
M. R. Yamsani

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.


2015 ◽  
Vol 7 (1-2) ◽  
pp. 65-74
Author(s):  
K. Latha ◽  
V. V. Srikanth ◽  
S. A. Sunil ◽  
N. R. Srinivasa ◽  
M. U. Uhumwangho ◽  
...  

The objective of this investigation is to study the applicability of gum karaya, the natural gum for the preparation and in vitro evaluation of losartan potassium, as Chronotherapeutic Drug Delivery System (ChDDS). The compression-coated timed-release tablets (CCT) containing losartan potassium in the core tablet were prepared by dry coating technique with different ratios of gum karaya as the outer coat. The parameters investigated were tensile strength, friability, in vitro dissolution studies and drug concentration. The optimized formulation was further characterized by powder XRD and FTIR to investigate interactions and no interactions observed. The tensile strength and friability of all the CCT were between 1.06-1.23 MN/m2 and < 0.3% respectively.  All the CCT showed a clear lag time before a burst release of drug. However, the lag time of drug release increased as the amount of gum karaya in the outer layer increased. For instance, the lag time of LGK1, LGK2, LGK3, LGK4, LGK5, LGK6 and LGK7 were 16, 10.5, 5.5, 3, 2, 1.5 and 0.5 hrs respectively.  The drug content of all the CCT was >98%. Formulation LGK3 was taken as an optimized formulation which can be exploited to achieve ChDDS of losartan potassium for the treatment of hypertension. 


Author(s):  
Sunitha M Reddy ◽  
Sravani Baskarla

This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.  


Author(s):  
SARIPILLI RAJESWARI ◽  
VANAPALLI SWAPNA

Microsponges (MSPs) are at the forefront of the rapidly developing field of novel drug delivery systems which are gaining popularity due to their use for controlled release and targeted drug delivery. The microsponge delivery system (MDS) is a patented polymeric system consisting of porous microspheres typically 10-25 microns in diameter, loaded with an active agent. They are tiny sponge-like spherical particles that consist of a myriad of interconnecting voids within a non-collapsible structure with a large porous surface through which active ingredient is released in a controlled manner. Microsponge also hold a certification as one of the potential approaches for gastric retention where many oral dosage forms face several physiological restrictions due to non-uniform absorption pattern, inadequate medication release and shorter residence time in the stomach. This type of drug delivery system which is non-irritating, non-allergic, non-toxic, can suspend or entrap a wide variety of substances, and can then be incorporated into a formulated product such as gel, cream, liquid or powder that is why it is called as a “versatile drug delivery system”. It overcomes the drawbacks of other formulations such as frequency of dosing, drug reaction, incompatibility with environmental condition. These porous microspheres were exclusively designed for chronotherapeutic topical drug delivery but attempt to utilize them for oral, pulmonary and parenteral drug delivery were also made. The present review elaborates about the multifunctional microsponge technology including its preparation, characterization, evaluation methods along with recent research and future potential.


2021 ◽  
Vol 16 (1) ◽  
Author(s):  
Chao Yan ◽  
Yue Jin ◽  
Chuanxiang Zhao

AbstractNanoparticles as drug delivery systems can alter the drugs' hydrophilicity to affect drug uptake and efflux in tissues. They prevent drugs from non-specifically binding with bio-macromolecules and enhance drug accumulation at the lesion sites, improving therapy effects and reducing unnecessary side effects. Metal–organic frameworks (MOFs), the typical nanoparticles, a class of crystalline porous materials via self-assembled organic linkers and metal ions, exhibit excellent biodegradability, pore shape and sizes, and finely tunable chemical composition. MOFs have a rigid molecular structure, and tunable pore size can improve the encapsulation drug's stability under harsh conditions. Besides, the surface of MOFs can be modified with small-molecule ligands and biomolecule, and binding with the biomarkers which is overexpressed on the surface of cancer cells. MOFs formulations for therapeutic have been developed to effectively respond to the unique tumor microenvironment (TEM), such as high H2O2 levels, hypoxia, and high concentration glutathione (GSH). Thus, MOFs as a drug delivery system should avoid drugs leaking during blood circulation and releasing at the lesion sites via a controlling manner. In this article, we will summary environment responsive MOFs as drug delivery systems for tumor therapy under different stimuli.


2020 ◽  
Vol 11 (2) ◽  
pp. 2505-2518
Author(s):  
Sindhuja Devaraj ◽  
Ganesh GNK

Nanoparticulate drug delivery system are the rapidly developing system, and nanoparticles are present in the size range of 1-100nm. Nanoparticles composed of various thermal, electrical, and optical property. Nanoparticles offers the potential advantages over the traditional dosage forms it is ascribable to the properties of nanoparticles. Nanoparticulate drug delivery system ensures the site-specific delivery of a drug(Targeting drug delivery) and aids in improving the efficacy of the new as well as old drugs and has the potential in crossing the various physiological barriers and also improves the therapeutic index of the drugs and increases the patient compliance. The objectives of this review is to classify the nanoparticles based on the different groups, surface properties of nanoparticles, describe the strategies of drug targeting, the necessity of nanoparticles their general method of preparation, different methods used in characterization, self- assembly and mechanism of drug release in a systemic manner. The potential advantages and limitations of various nanoparticulate drug delivery systems are also discussed elaborately.


Author(s):  
Tushar N. Sonawane ◽  
Pradip D. Dhangar ◽  
Sagar D Patil ◽  
Azam Z. Shaikh

Novel Drug Delivery Systems are one of the widely use delivery system in the presence scenario. Novel drug delivery system is a novel approach to drug delivery that addresses the limitations of the traditional drug delivery systems. In the form of a Novel Drug Delivery System an existing drug molecule can get a new life. The novel drug delivery system is Increases bioavailability and it Can be used for long-term treatments of chronic illness, Sustained maintenance of plasma drug levels as well as it Decreased adverse drug effects in the total amount of drugs required thus reducing side effects it Improved patient compliance due to reduction in number and frequency of doses required. There is less damage sustained by normal tissue due to targeted drug delivery. In this paper our main focus to give the throughout knowledge of some newer (Novel drug delivery system) to understand the concept of the Novel dossage form.


2018 ◽  
Vol 10 (2) ◽  
pp. 1 ◽  
Author(s):  
Revathy B. Menon ◽  
Lakshmi V. S. ◽  
Aiswarya M. U. ◽  
Keerthana Raju ◽  
Sreeja C. Nair

A novel drug delivery system is the one that ensures optimum dose at the right time, at the right location. Porphysomes are among those drug delivery systems. Porphysomes are a means of vesicular drug delivery systems. They are liposome-like structures composed completely of porphyrin lipid. The porphysomes encapsulates the active medicament in vesicular structure. They are having an aqueous core which can be loaded with the medicament. They have the capacity to destroy the disease tissues. They absorb the heat in the near infrared region and release this heat to destroy the diseased tissues. Porphysomes are having immense applications in the field of positron-electron therapy (PET), photoacoustic imaging, photothermal therapy etc. This review article discusses regarding the Porphysome-the drug delivery system, its advantages and disadvantages, composition, method of preparation, applications and various aspects related to the porphysomal drug delivery.


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