Oral Controlled Release Drug Delivery Research Articles

Cydonia oblonga-Seed-Mucilage-Based pH-Sensitive Graft Copolymer for Controlled Drug Delivery-In Vitro and In Vivo Evaluation.

The primary objective of this study was to assess the potential utility of quince seed mucilage as an excipient within a graft copolymer for the development of an oral-controlled drug delivery system. The Cydonia oblonga-mucilage-based graft copolymer was synthesized via a free radical polymerization method, employing potassium per sulfate (KPS) as the initiator and N, N-methylene bisacrylamide (MBA) as the crosslinker. Various concentrations of monomers, namely acrylic acid (AA) and methacrylic acid (MAA), were used in the graft copolymerization process. Metoprolol tartarate was then incorporated into this graft copolymer matrix, and the resultant drug delivery system was subjected to comprehensive characterization using techniques such as Fourier-transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). The swelling behavior of the drug delivery system was evaluated under different pH conditions, and in vitro drug release studies were conducted. Furthermore, pharmacokinetic parameters including the area under the curve (AUC), maximum plasma concentration (Cmax), time to reach Cmax (Tmax), and half-life (t1/2) were determined for metoprolol-loaded hydrogel formulations in rabbit plasma, and these results were compared with those obtained from a commercially available product. The key findings from the study include observations that higher concentrations of acrylic acid (AA) and Cydonia oblonga mucilage (CM) in the graft copolymer enhanced swelling, while the opposite trend was noted at elevated concentrations of methacrylic acid (MAA) and N, N-methylene bisacrylamide (MBA). FTIR analysis confirmed the formation of the graft copolymer and established the compatibility between the drug and the polymer. SEM imaging revealed a porous structure in the prepared formulations. Additionally, the swelling behavior and drug release profiles indicated a pH-sensitive pattern. The pharmacokinetic assessment revealed sustained release patterns of metoprolol from the hydrogel network system. Notably, the drug-loaded formulation exhibited a higher Cmax (156.48 ng/mL) compared to the marketed metoprolol product (96 ng/mL), and the AUC of the hydrogel-loaded metoprolol was 2.3 times greater than that of the marketed formulation. In conclusion, this study underscores the potential of quince seed mucilage as an intelligent material for graft-copolymer-based oral-controlled release drug delivery systems.

A Review on Techniques and Applications of Gastroretentive Drug Delivery System

A Controlled release dose forms have been widely utilized to enhance treatment with a number of significant medications. However, a number of physiological challenges, including the inability to control and localize the system within the target region of the gastrointestinal tract and the extremely changeable nature of the gastric emptying process, pose challenges to the development processes. The bioavailability and periods needed to reach peak plasma levels may be unpredictable as a result of this diversity. The goal of this review on gastro retentive drug delivery systems was to gather the most recent research with a special emphasis on the numerous gastro retentive technologies that have lately emerged as leading approaches in the area of site-specific oral controlled release drug delivery. We have included crucial elements in order to comprehend numerous physiological challenges to achieve stomach retention.

Gel Based Formulations in Oral Controlled Release Drug Delivery

Gel-based formulations may be classified as hydrogels, emulgels, and organogels or oleogels. This categorization depends on the polarity of the liquid component present in it. Hydrogels offer excellent potential to be used in oral drug delivery due to inherent biocompatibility, diversity of both natural and synthetic components. In particular, stimuli-responsive hydrogels can meet the physiological changes along the gastro intestinal tract to achieve site-specific, controlled release of protein, peptide and many other molecules for systemic treatment. There are many different techniques for the preparation of different sort of customized hydrogel. In recent years the popularity of oleogels is also in increasing order due to the easy method of preparation and inherent long-term stability of these products to provide the ideal drug delivery matrix. Oleogels are comprised of non-polar dispersion medium like fixed oil, mineral oil, organic solvents which are gelled with organogelator. Most of the studies on oleogels has been conducted on their use in food applications. Hydrogel and oleogel both have good acceptance in the field of oral drug delivery. This review work highlights brief description about both Hydrogels and Oleogels focusing their characteristics, advantages, disadvantages, application, some major techniques of the preparations and modifications of the same in oral drug delivery.

Raft Forming Systems: A Novel Approach to Gastric Retention


 Oral delivery of drug is the most preferable drug delivery due to the ease of administration, patient compliance and flexibility in the formulations. In recent era various technologies have been made in research and development of oral controlled release drug delivery system to overcome various physiological difficulties such as variation in gastric retention and emptying time. Conventional oral dosage forms pose low bioavailability problems due to their rapid gastric transition from stomach, especially in case of drugs which are less soluble at alkaline pH of intestine and locally acting drugs in stomach get rapidly emptied. So, frequency of dose administration in such cases is increased. Gastro retentive drug delivery system (GRDDS) is facing many challenges which can be overcome by upcoming newly emerging approach, raft forming systems (RFS). The present study provides valuable information and highlights advances in this raft forming system. Different types of smart polymers used for their formulation have also been summarized. The current review focuses on the mechanism, formulation development and evaluation aspects of the raft forming systems and also highlights parameters which may lead to response variations in altered physiological conditions are discussed as well.

Statistical design of experiment-based formulation development and optimization of 3D printed oral controlled release drug delivery with multi target product profile

Statistical design of experiment-based formulation development and optimization of 3D printed oral controlled release drug delivery with multi target product profile

Mini-Tablets versus Nanoparticles for Controlling the Release of Amoxicillin: In vitro/In vivo Study.

IntroductionControlling the drug release from the dosage form at a definite rate is the main challenge for a successful oral controlled-release drug delivery system. In this study, mini-tablets (MTs) and lipid/polymer nanoparticles (LPNs) of lipid polymer and chitosan in different ratios were designed to encapsulate and control the release time of Amoxicillin (AMX).MethodsPhysical characteristics and in vitro release profiles of both MT and LPN formulations were studied. Antimicrobial activity and oral pharmacokinetics of the optimum MT and LPN formulations in comparison to market tablet were studied in rats.ResultsAll designed formulations of AMX as MTs and LPNs showed accepted characteristics. MT-6 (Compritol/Chitosan 1:1) showed the greatest retardation among all prepared minitablet preparations, releasing about 79.5% of AMX over 8 h. In contrast, LPN-11 (AMX: Cr 1:3/Chitosan 1 mg/mL) had the slowest drug release, revealing the sustained release of 80.9% within 8 h. The MIC of both optimized tablet formula (MT-6) and LPNs formula (LPN-11) was around two-fold lower than the control against H. pylori. The Cmax of MT-6 and LPN11 were non significantly different compared with the marketed AMX product. While the bioavailability experiment proved that the relative bioavailability of the AMX was 1.85 and 1.8 after the oral use of LPN11 and MT-6, respectively, compared to the market tablet.ConclusionThe results verified that both controlled-release mini-tablets and lipid/polymer nanoparticles can be used for sustaining the release and hence improve the bioavailability of amoxicillin.

Formulation and Development of Extended Release Matrix Tablet of Carvedilol Phosphate

Carvedilol Phosphate, a non selective β-blocker drug under BCS class П and used in treatment of Hypertension. Solubility of the drug and its bioavailability is low. The purpose of the present study is to design extended release matrix tablet of Carvedilol Phosphate to improve gastric retention and reduce gastric emptying time. All blended formulations were evaluated for bulk density, tapped density, Carr’s index, angle of repose and the Hausner’s ratio. All these results indicated that, the powder blend showed good flow properties. All tablet formulations were evaluated for weight variation, hardness, Friability, Thickness, Content uniformity, In-vitro drug release. Regulated drug release in zero-order manner attained in the current study indicates that the optimized extended release tablet of Carvedilol Phosphate, prepared using Sodium carboxymethyl cellulose and HPMC K4M can successfully be employed in oral controlled release drug delivery system. Modified release ability of the formulation is likely to increase its GI residence time, and eventually, improve the extent of bioavailability.

Design of alpha mangostin-loaded chitosan/alginate controlled-release nanoparticles using genipin as crosslinker

α–Mangostin-loaded chitosan/alginate (CS/ALG) nanoparticles cross-linked with genipin (GP) were prepared for oral controlled drug release. A full factorial design was conducted to investigate the effects of the needle gauge, stirring rate and α–mangostin loading on the size of the nanoparticles. In order to provide controlled release, the nanoparticles were modified by crosslinking with GP, and the physical and chemical characteristics of the obtained systems were studied by FT-IR, PXRD and DSC. The α–mangostin loading and release was investigated, and the antitumour activity of nanoparticles was demonstrated. The results showed that small nanoparticles were obtained by maximising needle gauge and stirring rate and minimising the α–mangostin loading. A high α–mangostin loading and insignificantly larger particle size were observed with GP cross-linked nanoparticles. Moreover, GP nanoparticles acted as drug carriers sustaining α–mangostin release, which was slower at acidic pH compared to higher pH. These patterns were beneficial for α–mangostin release in the colon. Moreover, α–mangostin loaded GP nanoparticles exhibited antitumour activity against the colorectal cancer cells. These results suggest that GP nanoparticles could possibly be a good candidate for oral controlled release drug delivery to colon.

Oral Controlled Drug Delivery System-A Review

The new generation of oral controlled release drug delivery system technologies brings valuable benefits to patients. Oral route is the most convenient and commonly route of drug delivery. Oral controlled release formulations are designed to deliver a drug at a pre determined rate by achieving a constant drug level for a specified period of time with lower side effects. Controlled release drug delivery have become a significant priority worldwide, it may be possible to achieve rapid absorption of drug and increased bio availability, reduced toxicity and improved patient compliance. This article mainly focuses the requirement of controlled drug delivery system, their advantages, disadvantages, formulation, various methods and use of controlled release system.

Formulation, release characteristics, and bioavailability study of gastroretentive floating matrix tablet and floating raft system of Mebeverine HCl.

To prolong the residence time of dosage forms within the gastrointestinal tract until all drug is released at the desired rate is one of the real challenges for oral controlled-release drug delivery systems. This study was designed to develop a controlled-release floating matrix tablet and floating raft system of Mebeverine HCl (MbH) and evaluate different excipients for their floating behavior and in vitro controlled-release profiles. Oral pharmacokinetics of the optimum matrix tablet, raft system formula, and marketed Duspatalin® 200 mg retard as reference were studied in beagle dogs. The optimized tablet formula (FT-10) and raft system formula (FRS-11) were found to float within 34±5 sec and 15±7 sec, respectively, and both remain buoyant over a period of 12 h in simulated gastric fluid. FT-10 (Compritol/HPMC K100M 1:1) showed the slowest drug release among all prepared tablet formulations, releasing about 80.2% of MbH over 8 h. In contrast, FRS-11 (Sodium alginate 3%/HPMC K100M 1%/Precirol 2%) had the greatest retardation, providing sustained release of 82.1% within 8 h. Compared with the marketed MbH product, the Cmax of FT-10 was almost the same, while FRS-11 maximum concentration was higher. The tmax was 3.33, 2.167, and 3.0 h for marketed MbH product, FT-10, and FRS-11, respectively. In addition, the oral bioavailability experiment showed that the relative bioavailability of the MbH was 104.76 and 116.01% after oral administration of FT-10 and FRS-11, respectively, compared to marketed product. These results demonstrated that both controlled-released floating matrix tablet and raft system would be promising gastroretentive delivery systems for prolonging drug action.

A review on gastroretentive drug delivery system

Oral controlled release and site specific drug delivery system has been of great interest in pharmaceutical field to achieve improved therapeutic advantage. Concept of novel drug delivery system arose to overcome certain aspect related to physicochemical properties of drug molecule and the related formulations. Gastro retentive drug delivery system is one of such novel approaches to prolong gastric residence time, thereby targeting site specific drug release in the stomach for local or systemic effects. This approach is useful particularly for the drugs which have narrow absorption window in the upper part of gastro intestinal tract. In this review we have been discussed various approaches of gastro retentive drug delivery system, such as floating and non-floating systems.

Oral controlled release drug delivery system and Characterization of oral tablets; A review

Oral route of drug administration is considered as the safest and easiest route of drug administration. Control release drug delivery system is the emerging trend in the pharmaceuticals and the oral route is most suitable for such kind of drug delivery system. Oral route is more convenient for It all age group including both pediatric and geriatrics. There are various systems which are adopted to deliver drug in a controlled manner to different target sites through oral route. It includes diffusion controlled drug delivery systems; dissolution controlled drug delivery systems, osmotically controlled drug delivery systems, ion-exchange controlled drug delivery systems, hydrodynamically balanced systems, multi-Particulate drug delivery systems and microencapsulated drug delivery system. The systems are formulated using different natural, semi-synthetic and synthetic polymers. The purpose of the review is to provide information about the orally controlled drug delivery system, polymers which are used to formulate these systems and characterizations of one of the most convenient dosage form which is the tablets.

Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent

To prolong the residence time of dosage forms within gastrointestinal trace until all drug released at desired rate was one of the real challenges for oral controlled-release drug delivery system. Herein, we developed a fine floating tablet via compression coating of hydrophilic polymer (hydroxypropyl cellulose) combined with effervescent agent (sodium bicarbonate) to achieve simultaneous control of release rate and location of ofloxacin. Sodium alginate was also added in the coating layer to regulate the drug release rate. The effects of the weight ratio of drug and the viscosity of HPC on the release profile were investigated. The optimized formulations were found to immediately float within 30s and remain lastingly buoyant over a period of 12h in simulated gastric fluid (SGF, pH 1.2) without pepsin, indicating a satisfactory floating and zero-order drug release profile. In addition, the oral bioavailability experiment in New Zealand rabbits showed that, the relative bioavailability of the ofloxacin after administrated of floating tablets was 172.19%, compared to marketed common release tablets TaiLiBiTuo®. These results demonstrated that those controlled-released floating tables would be a promising gastro-retentive delivery system for drugs acting in stomach.

Interpolyelectrolyte complexes of Eudragit® EPO with hypromellose acetate succinate and Eudragit® EPO with hypromellose phthalate as potential carriers for oral controlled drug delivery.

The objective of this study was to compare a novel controlled release tablet formulation based on interpolyelectrolyte complex (PEC). Interpolymer interactions between the countercharged polymers like Eudragit® EPO (polycation) and hypromellose acetate succinate (polyanion) and Eudragit® EPO and hypromellose phthalate (polyanion) were investigated with a view to their use in per oral controlled release drug delivery systems. The formation of inter-macromolecular ionic bonds between cationic polymer and anionic polymer was investigated using Fourier transform infrared (FT-IR) spectroscopy and differential scanning calorimetry. The FT-IR spectra of the tested polymeric matrices are characterized by visible changes in the observed IR region indicating the interaction between chains of two oppositely charged copolymers. The performance of the in situ formed PEC as a matrix for controlled release of drugs was evaluated, using acetaminophen as a model drug. The dissolution data of these matrices were fitted to different dissolution models. It was found that drug release followed zero-order kinetics and was controlled by the superposition of the diffusion and erosion. These profiles could be controlled by conveniently modifying the proportion of the polymer ratio, polymer type, and polymer concentration the in the tablets.

Formulation Development and Evaluation of Gastro-Retentive Drug (Torsemide) Delivery System for Diuretic Drug

Gastro-retentive Drug Delivery System is system which improves the Gastric Residence time and hence improves its bioavailability. In the current study indicates that the optimized gastro-retentive tablet of Torsemide, prepared using Sodium Alginate and HPMC K15M can successfully be employed as an oral controlled release drug delivery system. Tablet was formulated by using different Formulation indicated by F1 to F9 respectively. These formulations were evaluated for the pre compression and post compression parameters. The optimized Formulation was subjected to stability studied at 40oC under humidity conditions (75%) for a period of four week. From the result it was observed that there was no significant change in physiochemical properties as well as in drug release profile even after storage at 40oC for four week. In-vitro drug release study of formulation also done for optimized batch after stability study and found unaffected. High floating ability of the formulation is likely to increase its GI residence time, and eventually, improve the extent of bioavailability. Gastroretentive dosage form of Torsemide will reduce the frequency of administration of drug and helps to minimize dose of drug and side effects associated with the drug.

Optimizing Oral Controlled Release Drug Delivery Systems Using Experimental Designs

Optimizing Oral Controlled Release Drug Delivery Systems Using Experimental Designs

Optimizing Oral Controlled Release Drug Delivery Systems using Experimental Designs

The number of literature reports on the use of design of experiments optimization in development of drug delivery technology has been piling up steadily. This review article provides an updated bird’s eye view survey account on the publications and optimization techniques of different novel controlled release delivery designs for use in oral applications. Such systematic techniques find their use in every type of conventional dosage form and novel drug delivery system. The drug delivery devices investigated for optimization using various designs include oral controlled release tablet. The present manuscript deal with various steps involved in design of experiments optimization methodology using diverse experimental designs. It also deals with a variety of showing literature findings as well as the potential application of such design of experiments procedures on optimization of assorted drug delivery systems. Such an explicit and updated review on drug delivery optimization has not been published anywhere else in the recent past.

PATENTED PHARMACEUTICAL ORAL CONTROLLED RELEASE MATRIX SYSTEM

Abstrac t Oral controlled release drug delivery system becomes a very promising approach for those drugs that are given orally but having the high dosing frequency and shorter half - life. Matrix tablets serves as an important tool for oral controlled release dosage forms. Problems like patient compliance, drug targeting, local side effects, frequent administration and fluctuations in blood concentration levels, associated with their counterparts, the conventional dosage forms were rectified. Many of the pharmaceutic al dosage form are formulated as sustained release dosage form to retard the release of a therapeutic agent such that its appearance in the systemic circulation is prolonged and its plasma profile is sustained in duration. Tablets offer the lowest cost app roach to controlled and sustained release dosage forms. Matrix tablet as controlled release has given a new breakthrough for novel drug delivery system in the field of pharmaceutical technology. This review focuses on the various types of matrix systems ba sed on polymer used and porosity of matrix system i.e. hydrophilic, hydrophobic, fat wax, porous, non - porous, pH sensitive. An effort has been made to consolidate different types of patents granted across the globe for last thirty years in the field of mat rix system viz. tablet, pellets etc.

Stimuli-responsive bacterial cellulose-g-poly(acrylic acid-co-acrylamide) hydrogels for oral controlled release drug delivery

This study evaluated the potential of stimuli-responsive bacterial cellulose-g-poly(acrylic acid-co-acrylamide) hydrogels as oral controlled-release drug delivery carriers. Hydrogels were synthesized by graft copolymerization of the monomers onto bacterial cellulose (BC) fibers by using a microwave irradiation technique. The hydrogels were characterized by Fourier transform infrared (FT-IR) spectroscopy, X-ray diffraction (XRD), thermogravimetric analysis (TGA) and scanning electron microscopy (SEM). FT-IR spectroscopy confirmed the grafting. XRD showed that the crystallinity of BC was reduced by grafting, whereas an increase in the thermal stability profile was observed in TGA. SEM showed that the hydrogels exhibited a highly porous morphology, which is suitable for drug loading. The hydrogels demonstrated a pH-responsive swelling behavior, with decreased swelling in acidic media, which increased with increase in pH of the media, reaching maximum swelling at pH 7. The release profile of the hydrogels was investigated in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). The hydrogels showed lesser release in SGF than in SIF, suggesting that hydrogels may be suitable drug carriers for oral controlled release of drug delivery in the lower gastrointestinal tract.

ORAL CONTROLLED RELEASE DRUG DELIVERY SYSTEM: AN OVERVIEW

Oral drug delivery is the most preferred and con venient option as the oral route provides maximum active surface area among all drug delivery system for administration of various drugs. The attractiveness of these dosage forms is due to awareness to toxicity and ineffectiveness of drugs when administere d by oral conventional method in the form of tablets and capsules. Usually conventional dosage form produces wide range of fluctuation in drug concentration in the bloodstream and tissues with consequent undesirable toxicity and poor efficiency. The mainte nance of concentration of drug in plasma within therapeutic index is very critical for effective treatment. These factors as well as factors such as repetitive dosing and unpredictable absorption lead to the concept of oral controlled release drug delivery systems. Controlled release drug delivery system works on many different mechanisms to control the release rate of drugs. Various mechanisms like osmotic pressure, matrix system, reservoir system, altered density system etc. have been utilized as formulat ion approaches. The present article contains brief review on various formulation approaches for controlled release drug delivery system.