Pulsatile Drug Delivery System Research Articles

Formulation and Evaluation of Pulsatile Drug Delivery System for the Treatment of Arthritic Pain

Formulation and Evaluation of Pulsatile Drug Delivery System for the Treatment of Arthritic Pain

DEVELOPMENT AND OPTIMIZATION OF RABEPRAZOLE CHRONO-MODULATED DRUG DELIVERY SYSTEMS

Objective: Development and optimization of chrono-modulated pulsatile drug delivery systems (CPDDS) loaded with Rabeprazole for treating nocturnal acid breakthrough in ulcer patients was set as the major objective of this work. Methods: CPDDS were developed to provide drug release as two pulses with predetermined gap. Separate microparticles for delayed instant release (DIR) and delayed extended-release (DER) were formulated. Through the optimization of several formulation and process parameters, ER microparticles were created as matrix microspheres. Central composite design was used to understand how the factors affected the responses. The optimized ER microspheres and plain drug were separately subjected to enteric coating to obtain DER and DIR portion microparticles, respectively. Results: With the exception of stirring speed's impact on drug release, every other factor was found to have a significant influence (p<0.05) on every response. The mechanism underlying the Rabeprazole's delayed prolonged release was explained by the SEM images. The microspheres made with Eudragit RSPO at 0.72 g and polyethylene oxide at 0.5 g for 1 g of Rabeprazole at 400 rpm were shown to be the optimal formulation based on the graphical optimization results. After being coated with a terminal enteric coating, this formulation showed delayed release for a duration of 6 h. Conclusion: After oral administration of equal doses of DIR microcapsules along with the optimized DER microspheres could release Rabeprazole effectively as two different pulses at the desired time intervals.

Pulsatile Drug Delivery Systems: A Comprehensive Review

sigmoidal drug release profile is formed when a pulsatile drug delivery system (PDDI) initiates drug administration and follows it up with rapid and complete drug release. It ensures the correct dosage of the drug is delivered at the right time and place. Pulsatile drug delivery is effective for treating asthma, arthritis, cancer, diabetes, epilepsy, hypertension, ulcers, and hypercholesterolemia, among others. There are many types of delivery systems in the pharmaceutical industry, including capsular, osmotic, single and multi-unit designs and membranes that are soluble and erodible. Innovations are directed toward conditions such as those requiring nocturnal dosing, high first-pass effects, and site-specific absorption in the gastrointestinal tract. In particular, these systems make dosing more convenient for patients, resulting in better compliance. As a result of the use of chronomodulated drug delivery systems, pharmaceutical therapy is more effective with a personalized approach.

Formulation and Evaluation of Bioadhesive Pulsatile Drug Delivery System of an Antihypertensive Drug

Formulation and Evaluation of Bioadhesive Pulsatile Drug Delivery System of an Antihypertensive Drug

FORMULATION AND EVALUATION OF MODIFIED PULSATILE CAPSULE FOR CHRONOPHARMACOTHERAPY OF RHEUMATOID ARTHRITIC PAIN

Objective: The objective of the present study was to design and evaluate pulsincap system for chrono pharmacotherapy of rheumatoid arthritis that combines advantages of both immediate and sustained release technology with the suitable delay of drug release. Methods: Pulsatile drug delivery system based on pulsincap® technology was designed using mucoadhesive microspheres and Tramadol bilayer tablet plugs. The drug-excipient interaction was carried out by FTIR. Hardness, thickness, lag time, and swelling index all play a role in optimizing tablet plugs. The microspheres were examined for parameters such as particle size, surface morphology, encapsulation efficiency, swelling index, % mucoadhesion, and in vitro dissolution. Results: In modified pulsincaps, bilayer tablet plug shows drug release within 40 min and hydrogel plugs shows good swelling index and suitable lag time. In microspheres formulations, MF9 is the most suitable among them as it shows better drug content, particle size, surface morphology, in vitro drug release, and release kinetics. The drug is released right away, followed by the dissolution of the enteric coating at pH 6.8, followed by a suitable delay of 6 hours, and then the maximum amount of drug release is 99.62% at the end of 10th h. Conclusion: The pulsatile delivery system developed with HPMCK4M and tamarindus gum as plugging material showed a satisfactory lag period when compared to Tamarindus gum alone. Drug release can be achieved from treated gelatin capsule and hydrogel plug for a prolonged period by MF9 formulation.

Design, Evaluation and Optimization of Albuterol Sulphate and Theophylline Pulsincap drug delivery system for chronotherapy of Asthma

The aim of the current study was to design and develop and evaluate pulsatile drug delivery system of Albuterol Sulphate and Theophylline for the treatment of Asthma. The capsule body was made water insoluble by cross linked with formaldehyde vaopur. The treatment of Formalin was adopted to modify the gelatin capsule solubility. The formalin residue was carried out by quantitative test. The drug-excipient compatibility is done by FTIR and UV . The pulsincap formulation were prepared by using hydrogel plug of various components. The drug content of the formulation of pulsincap was found to be in the general range. The invitro drug release studies in ph1.2 .6.2 and 7.4 buffern was noticed to be zero percent and capsule was stable for 2 hours drug the studyF5 formulation batch was selected which was best and good formulation and promoted maximum drug release of 96.29% percentage at phosphate buffers when compared with other formulation. Pulsincap formulation can be adopted for optimum delivery of pellets in the treatment as per chronotherapy
 Keywords: Theophylline, quantitative test, invitro drug release studies, phosphate buffers6.2 and 7.4.

PULSATILE DRUG DELIVERY SYSTEMS THE NOVEL APPROACH

Oral pulsatile drug delivery systems (PDDS) are intended to induce programmable lag phases before a quick and quantifiable, repeated, or prolonged medication release. As a result, they are gaining popularity due to their inherent suitability for achieving chronotherapeutic goals, which have just been highlighted concerning several prevalent chronic illnesses characterized by typical night or early-morning recurring symptoms (e. g. bronchial asthma, heart attack, rheumatoid arthritis, early-morningawakening). Furthermore, time-based colonic release is possible when pulsatile delivery devices are correctly modified to overcome unexpected gastric emptying and give delay periods that roughly match the small intestine transit time. Oral pulsatile administration is accomplished using several release platforms, including reservoir, capsular, and osmotic devices. The current review article addressed the topics that followed: the reason pulsatile drug delivery systems have been invented; diseases for which pulsatile release is necessary; classification, advantages and disadvantages; methods used in the current systems; the situation nowadays and its potential for the future; recent advancements, and especially, the previous five to ten years of research on pulsatile drug delivery conducted by researchers using a variety of drugs for a variety of diseases.

Pulsatile Drug Delivery System: A Review

Abstract: The pulsatile drug delivery system has carried off a lot of importance in drug delivery technology in the last 30 years the aim of the present work was to formulate and evaluate an oral pulsatile drug delivery system to achieve time release of melonixcam, based on chronopharmaceutical approach for the treatment of anti-inflammatory agent. Thus drug can be delivered at righttime, in right amount and at right site of action by use of such approach. A pulse must be planned sothat a complete and rapid medication release is accomplished after the lag time. Holds good promises and provides benefit to the patients suffering from chronic problems like arthritis, asthma, hypertension etc.

Chronomodulated drug delivery systems for the treatment of hypertension: An overview

This review paper aims to provide an overview of chronomodulated drug delivery systems for the treatment of hypertension. Hypertension is a chronic medical condition that affects millions of people worldwide, and effective treatment is crucial to prevent complications such as heart disease and stroke. Chronomodulated drug delivery utilises the concept of circadian rhythms to optimise drug efficacy and minimise side effects. The paper examines various chronomodulated drug delivery approaches, including pulsatile, delayed-release, and chronopharmaceutical systems, highlighting their advantages and limitations. Furthermore, the potential future developments in this field are discussed, emphasising the importance of personalised medicine and the integration of wearable technology for real-time monitoring and drug administration. Overall, this review provides valuable insights into the potential of chronomodulated drug delivery systems for improving patient outcomes and minimising side effects. By utilising chronomodulated drug delivery approaches, healthcare professionals can ensure that medications are released at specific times when they are most effective, thereby maximising their therapeutic benefits. Pulsatile drug delivery systems, for example, can mimic the body's natural circadian rhythm, allowing for targeted drug release during periods of peak efficacy. Delayed-release systems, on the other hand, can help reduce side effects by delivering drugs to specific regions of the gastrointestinal tract where they are better tolerated.

Formulation and in-vitro evaluation of floating pulsatile drug delivery of chronotherapeutic release of h2 receptor antagonist of famotidine

In the present study famotidine floating pulsatile drug delivery system was developed. Various type and different concentrations of superdisintegrants and polymer affect the drug release. FTIR studies concluded that there is no interaction between drug and excipients. Based on disintegration time and dissolution time the formulation (F2) which contains 8% sodium starch glycollate was optimised. The optimised formulation F2 was further coated with different concentrations of HPMC K4M,HPMC K 15M and HPMC K 100M..Based on the concentration of the coating layer and solubility of the coating layer and the dissolution data the formulation (F6) which was coated with 150mg of HPMC K 15M was optimised.

QbD: A novel approach for formulation and optimization of colon targeted drug delivery system containing mebeverine HCl

The aim of the work is to study the programmed release of model antispasmodic drug Mebeverine HCl based on pulsatile principle to target colon proximity. Compression coated tablets included core tablet consisting of Croscarmellose as super disintegrant and pulsatile layer comprising impermeable Ethocel cup and mixture of Keltone, Eudragit S100, Ethocel as swellable and rupturable layer. The prepared core tablet was evaluated for weight variation, hardness, thickness, friability, drug content, disintegration time and in vitro dissolution studies. For optimization Box-Behnken design was employed to study the effect of independent variables viz., weight ratio of Keltone (X1), Eudragit S100 (X2), Ethocel (X3) on dependent variables viz., t10 (Y1), t50 (Y2) and Q12 (Y3). Results revealed positive influence of independent factors on responses. The data were statistically analyzed using ANOVA and were found to be statistically significant (P < 0.05). Mathematical modeling for kinetic studies revealed that the release profile after lag time followed first order kinetics. The results concluding that a successful pulsatile drug delivery system of Mebeverine HCl was developed.

Formulation and Evaluation of Pulsatile Drug Delivery System of Dexlansoprazole

Background: A pulsatile drug delivery system is intended to deliver drugs according to the circadian rhythm, or disease cycle. PDDS prepared by pulsincap technology contain a cross-linked hard gelatin capsule filled with the optimized immediate-release tablet, sodium alginate beads. Dexlansoprazole is used to treat the signs and symptoms of gastroesophageal reflux disease (GERD), erosive esophagitis, and stomach ulcers. Objective: The objective of the research is to develop and analyse a controlled-release pulsatile medication delivery system for the treatment of peptic ulcers that contains dexlansoprazole. Method: The Pulsincap system consists of a hard gelatin capsule containing an immediate-release tablet prepared by direct compression, sodium alginate beads prepared by the ionotropic gelatin method, and a hydrogel plug made through direct compression. The hydrogel plug was prepared by using various grades of HPMC polymer. The immediate-release tablet was prepared by direct compression. Result: The results of the present FTIR studies concluded that there was no interaction between dexlansoprazole and the excipient. Based on the evaluation parameter, it was found that the F2 tablet (1:2) ratio and 2% sodium alginate beads showed better results. Polymer HPMC K15M for Hydrogel showed the desired swelling time. Conclusion: It was concluded that the preparation of a pulsatile drug delivery system for dexlansoprazole through pulsincap technology can give drug release in a pulsed manner that is first immediate release, lag time, and sustain action.

Preparation and evaluation of press coated floating pulsatile drug delivery system of telmisartan

The aim of present investigation was to develop press coated tablets for Floating pulsatile drug delivery of Telmisartan used for is a medication used for high blood pressure, heart failure, and diabetic kidney disease. The drug delivery system was designed to deliver the drug such a time when it could be needful of patient conditions. The press coated tablets containing Telmisartan in the inner core were formulated by direct compression method with an outer coating of different amount of Chitosan. The release profile of press coated tablet exhibited a lag time. The optimized batch F9 gave good drug release of 99.58 %

PULSATILE DRUG DELIVERY: A STRATEGY FOR TREATING CHRONOTHERAPEUTIC AILMENTS

Modern drug delivery systems have been promoted to a unique notion of chronopharmacology, i.e., the ability to provide the medicament to a patient in a staggered profile, as the discipline of chronobiology has advanced. The main disadvantage of developing such a delivery system that fits the circadian cycle is the lack of accurate technology (Pulsatile drug delivery system, PDDS). Pulsatile devices are gaining popularity because they deliver the medicine to the correct region of action at the correct time, allowing for spatial and temporal dosing and compliance among patients. These technologies are meant to work with the body's natural circadian cycle. The circadian rhythm affects various biological systems in humans, including metabolism, physiology, behaviour, sleep patterns, hormone synthesis, and so on. This article addresses several methods, such as osmotic systems, capsular systems, single and multiple-unit programable devices that rely on soluble or erodible polymer coatings, and the usage of rupturable membranes. The present review covered the rationale for the creation of pulsatile drug delivery systems, benefits, limitations the types of diseases that require pulsatile release, categorization, and assessments of pulsatile system of drug delivery.

Structural Aspect of Hydroxyethyl-Starch–Anticancer-Drug-Conjugates as State-of-the-Art Drug Carriers

Cancer is a genetic disorder and its treatment usually requires a long time and expensive diagnosis. While chemotherapy is the most conventional approach in treating most cancers, patients often suffer from undesired side effects due to various pharmacokinetic aspects. To address this issue, target-oriented drug-delivery systems (DDS) or pulsatile drug-delivery systems (PDDS) have recently been developed as an alternative tool that takes care of the entire pharmacodynamic activities of drug action. Hydroxyethyl starch (HES) has emerged as an effective clinical tool for delivering anticancer agents into target cells. These systems have demonstrated significant potential as anticancer drug carrier conjugates through their innate pharmacokinetic properties with their safety profile. This review focuses primarily on the structural aspect during the use of HES or HES-based polymers as carriers for delivering well-known anticancer drugs. This review also indicates a perspective on the long-term research needed for the sake of improving modern drug-delivery systems based on HES polymers and in the form of nanocarriers.

A Review on Pulsatile Drug Delivery System

In essence, pulsatile drug delivery systems (PDDS) are time-controlled drug delivery systems in which the system regulates the lag time independently of external parameters such as pH, enzymes, gastro-intestinal motility, etc. Traditionally, medications either release immediately or over time. Nevertheless, interest in pulsatile drug release devices has grown recently. These systems were created to work with the body's natural circadian cycle. In Latin literature, Circa and Dian are the words for day and night, respectively. For many medications or treatments, pulsatile drug release—in which the drug is released quickly after a clearly defined lag—could be useful. Asthma, peptic ulcer, cardiovascular disease, arthritis, attention deficit disorder in children, and hypercholesterolemia are among the illnesses where PDDS appears promising. This medication distribution system has been pre-programmed

A Scalable Platform for Fabricating Biodegradable Microparticles with Pulsatile Drug Release.

Pulsatile drug delivery systems have the potential to improve patient adherence and therapeutic efficacy by providing a sequence of doses in a single injection. Herein, a novel platform, termed Particles Uniformly Liquified and Sealed to Encapsulate Drugs (PULSED) is developed, which enables the high-throughput fabrication of microparticles exhibiting pulsatile release. In PULSED, biodegradable polymeric microstructures with an open cavity are formed using high-resolution 3D printing and soft lithography, filled with drug, and sealed using a contactless heating step in which the polymer flows over the orifice to form a complete shell around a drug-loaded core. Poly(lactic-co-glycolic acid) particles with this structure can rapidly release encapsulated material after delays of 10 ± 1, 15 ± 1, 17 ± 2, or 36 ± 1 days in vivo, depending on polymer molecular weight and end group. The system is even compatible with biologics, releasing over 90% of bevacizumab in its bioactive form after a two-week delay in vitro. The PULSED system is highly versatile, offering compatibility with crystalline and amorphous polymers, easily injectable particle sizes, and compatibility with several newly developed drug loading methods. Together, these results suggest that PULSED is a promising platform for creating long-acting drug formulations that improve patient outcomes due to its simplicity, low cost, and scalability.

Formulation and Evaluation of Bosentan Pulsatile Drug Delivery System by using Press Coated Technique

In the present research work, we have designed a pulsatile formulation of Bosentan to treat High blood pressure as per the chronotherapeutic pattern of the disease. Core tablets were prepared by incorporating different concentration of disintegrants and were compressed in between different concentration of polymers. The core and compression coated tablets were subjected to pre-formulation, physicochemical and In-vitro drug release studies. FTIR studies revealed that there was not any chemical reaction between pure drug Bosentan and polymers. The pre and post-compressional parameters of tablets were also found to be within limits. Our optimized formulation F-6 releases Bosentan after a lag time of 2 hours and 98.01 % up to 12 hours. Formulations were stable for at least 3 months under standard long-term and accelerated storage conditions.

Present scenario of pulsatile drug delivery system

In current years, pulsatile drug release systems (PDRS) are ahead raising attention as compared to conventional drugs. In this delivery system, the drug is liberate quickly after a well defined insulate-time, could be helpful for many medicines or treatments. It can be labeled in single and a couple of-pulse structures. Other structures consist of a drug-enclosed core, enclosed by means of a swelling layer and an outer layer is insoluble, however coating with semipermeable polymer. The lag time earlier to the rupture is specifically controlled via: the penetration and mechanical houses of the coated polymer and the behaviour of swelling depend on the swelling layer. As is within the residing frame frequently observed that, many fundamental capabilities are regulated with the aid of brief or pulsed launch of bioactive substances at a precise site and time. Therefore its miles grave to expand novel drug transport systems to attain pulsed launch of a sure amount of medicine a good way to imitate the feature of the dwelling systems, whilst reduce undesirable side results. Particular interest has been given to the thermally receptive poly (N-isopropylacrylamide) and its imitative hydrogels. Pulsatile drug transport is a machine that, by means of handing over drug at the right vicinity, right amounts and in proper time, grips suitable assures of benefit to the patients affected by continual problems like high blood pressure, allergies, arthritis.

Exploration of polymethacrylate and Hypromellose for the development of a non-sulfhydryl ACE inhibitor mucoadhesive system using Box-Behnken design: in-vitro and ex-vivo evaluation

Purpose To counteract early morning pathology like hypertension a time-dependent release of the drug is required. This study is focused to formulate a pulsatile and mucoadhesive drug delivery system of an ACE inhibitor Perindopril Erbumine. Method Two matrix tablets were punched with Eudragit RSPO, Eudragit RLPO, and HPMC K15M using a 3-3-3 Box-Behnken Design of Response Surface Methodology. Based on the design-optimized formulation P1T3 and P2T8 were coated for a lag time with compression coating of HPMC K4M and a blend of 1:1 ratio of ethylcellulose and carbopol polymer and further encapsulated in a Eudracap™ capsule to provide gastric resistance. Result The in-vitro release data confirmed an initial pause phase of 4.5 h then release of the drug for 5.2 ± 0.3 h to cope with the early morning rush in blood pressure. After that, a gap of 6 h and then sustained release of the drug for 10.5 ± 0.5 h. From the ex-vivo study, mucoadhesive strength was obtained as 55.13 ± 0.03 gm and 56.39 ± 0.02 gm for P1T3 and P2T8 respectively. The lag time for coated tablet P1T3 came to 2.15 ± 0.15 h and for P2T8 11.9 ± 0.10 h proving the coating efficiency of polymers. Conclusion The current study strongly suggests that perindopril Erbumine in association with Eudragit and Hypromellose polymer can open a path for the time-regulated release of the drug for hypertension chronotherapy with less risk of dose dumping.