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116EXPLORING INNOVATIVE STRATEGIES FOR DEVELOPING FLOATING DRUG DELIVERY SYSTEMS: AN EXTENSIVE REVIEW
Sangu Jyothi
Asst. Professor, Department of Pharmaceutical Chemistry, Princeton College of Pharmacy, Hyderabad, Telangana, India
Roopani Madhu
Asst. Professor, Department of Pharmaceutical Chemistry, Princeton College of Pharmacy, Hyderabad, Telangana, India
Abstract - Currently, floating drug delivery systems (FDDS), swelling and expanding systems, polymeric bioadhesive systems, highdensity systems, modified-shape systems, and other delayed gastric emptying devices are used to extend the GRT. The most recent and current developments in stomach-specific FDDS are discussed in this review. Poor absorption occurs when drugs have a limited window of absorption in the gastrointestinal tract. As a result, gastroretentive drug delivery systems (GRDDS) have been developed to extend the time it takes for the stomach to empty. Floating drug delivery systems, raft systems, mucoadhesive systems, high density systems, superporous hydrogels, and magnetic systems are some of the methods that have been used. This audit additionally sums up the in vitro procedures, in vivo examinations to assess the presentation and use of drifting frameworks, and utilizations of these frameworks. The primary objective of this review of floating drug delivery systems (FDDS) was to compile the most recent research, with a particular focus on the principal mechanism by which floatation is used to achieve gastric retention.
Keywords: Floating drug delivery systems, gastrointestinal tract, mucoadhesive systems.
1 INTRODUCTION
These new drug delivery systems' most important goals are: In the beginning, it would be a single dose, which spreads out the active ingredient over a longer time period. Second, it ought to deliver the active substance directly to the site of action, thereby minimizing or eliminating any adverse effects. Floating tablets have been developed to overcome the limitations of the conventional drug delivery system. Poor absorption will occur for medications that have a limited window of absorption in the gastrointestinal tract (GIT).
Gastroretentive drug delivery systems have the advantage of extending the gastric emptying time for these medications. Floating drug delivery systems are one of the current methods used to create a successful stomach- specific or gastroretentive drug delivery system1. It has been frequently observed that drugs that are easily absorbed from the gastrointestinal tract have short
halflives and are quickly eliminated from the systemic circulation, resulting in drug absorption from the upper small intestine being incomplete. The development of oral sustained-controlled release formulations is an attempt to slowly release the drug into the GI tract, which helps to maintain an effective drug concentration in the systemic circulation for a longer period of time. A controlled-release drug delivery system is capable of achieving the benefits of maintaining the optimal therapeutic drug concentration in blood with predictable and reproducible release rates for an extended period of time; this is necessary to achieve appropriate therapeutic activity. enhancement of long- term activity for drugs with short half- lives; the absence of side effects; reducing drug waste and dosage frequency;
enhanced treatment and enhanced patient compliance, Understanding the three components of the system is
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117 necessary for the successful developmentof oral controlled drug delivery systems.
1. The drug's physiological and chemical properties
2. The GIT's anatomy and physiology, as well as the characteristics of the dosage forms
2 FLOATING DRUG DELIVERY SYSTEMS AND ITS MECHANISM
Because FDDS have a bulk density that is lower than that of gastric fluids, they can remain buoyant in the stomach for an extended period of time without affecting the rate at which the stomach empty.
While the framework is drifting on the gastric items the medication is delivered gradually at the ideal rate from the framework. The stomach expels the remaining system following the drug's release. As a result, GRT rises and plasma drug concentration fluctuations are better managed. However, in order for the dosage form to remain consistently buoyant on the surface of the meal, a minimal level of floating force (F) is also required, in addition to a minimal gastric content. A novel apparatus for determining the resultant weight has been described in the literature for measuring the floating force kinetics. The apparatus works by continuously measuring the force F, which is the force necessary to maintain the submerged object over time.
If F is higher on the positive side, the object will float better. In order to avoid the negative effects of unanticipated intragastric buoyancy capability variations, this apparatus contributes to the optimization of FDDS with regard to the stability and durability of the produced floating forces.
2.1 Approaches to Gastroretention Several techniques are reported in the literature to increase the gastric retention of drugs.
Systems with a High Density: These systems, which have a density of less than 3 g/cm3, are able to withstand the peristaltic movements of the stomach and
remain in the rogue18, 20. The main significant downside with these frameworks is that it is in fact challenging to fabricate them with a lot of medication (>50%) and accomplish required thickness of 2.4‐2.8g/cm. For the production of such a high-density formulation8, diluents like zinc oxide, titanium oxide, barium sulfate (density=4.9), and iron powder are required.
Systems of swelling and expansion: Due to their propensity to remain plugged in the pyloric sphincters, these systems are also referred to as "Plug type systems."
Even when fed, these polymeric matrices remain in the gastric cavity for several hours12.
Including Excipients with a Delay in Time: Feeding digestible polymers or fatty acid salts that charge the motility pattern of the stomach to a fed stage, thereby reducing the gastric emptying rate and permitting significant prolongation of the drug release, is another approach of interest for delayed gastric emptying.
Prolongation of GRT of medication conveyance framework comprises of consolidating deferring excipients like trietanolamine myristate in a conveyance system14.
Systems that Float: Because FDDS have a bulk density that is lower than that of gastric fluids, they can remain buoyant in the stomach for an extended period of time without affecting the rate at which the stomach empty. The drug is slowly released from the system at the desired rate while the system is floating on the contents of the stomach. The stomach expels the remaining system after the drug has been released18. A floating chamber filled with vacuum, air, or inert gas can be used to float a drug delivery system in the stomach.
3 CLASSIFICATION OF FLOATING DRUG DELIVERY SYSTEMS (FDDS) Floating drug delivery systems are classified depending on the use of 2
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118 formulation variables: effervescent andnoneffervescent systems.
Forms of effervescent, floating dosage:
Swellable polymers like methylcellulose and chitosan and various effervescent compounds like sodium bicarbonate, tartaric acid, and citric acid are used to create these matrix-type systems. They are made so that when they come into contact with the acidic contents of the stomach, CO2 is released and gets stuck in swollen hydrocolloids, giving the dosage forms buoyancy.
Ichikawa et al. came up with a novel floating dosage system that can be used for a variety of conditions. It is made up of effervescent layers and swellable membrane layers that are coated on sustained release pills. To keep the tartaric acid and sodium bicarbonate from coming into direct contact with one another, the inner layer of effervescent agents was divided into two sublayers. A swellable polymer membrane made of purified shellac and polyvinyl acetate surrounded these sublayers. This system settled down after being immersed in the buffer at 37 degrees Celsius, and the outer swellable membrane allowed the solution to enter the effervescent layer.
The neutralization reaction between the two effervescent agents resulted in the production of CO2 and balloon-like swollen pills with a density of less than 1.0 g/mL. It was discovered that the system had good floating ability regardless of pH or viscosity and that the drug (para-amino benzoic acid) released continuously.
Choi et al. used gasforming agents (calcium carbonate and sodium bicarbonate) to make floating alginate beads and studied how CO2 changed the physical properties, morphology, and release rates. The size, floating ability, pore structure, morphology, release rate, and mechanical strength of the floating beads were all significantly influenced by the type and quantity of gasforming agent used, according to the study. It was determined that calcium carbonate
produced beads that were both smaller and more durable than sodium bicarbonate. While sodium bicarbonate outperformed calcium carbonate as a gas- forming agent, calcium carbonate produced superior floating beads that allowed for better rate control of drug release.
3.1 Non-Effervescent Floating Dosage Forms
Polysaccharides, gel-forming or swellable cellulose hydrocolloids, and matrix- forming polymers like polycarbonate, polyacrylate, polymethacrylate, and polystyrene are utilized in non- effervescent floating dosage forms. The drug and the gel-forming hydrocolloid are thoroughly mixed in a straightforward manner as part of the formulation method. This dosage form expands when it comes into contact with gastric fluids after oral administration and reaches a bulk density of G 1. The dosage form is buoyant because of the air that is trapped within the swollen matrix. The gelatinous mass's swelling gel-like structure serves as a reservoir and allows for sustained drug release.
Nur and Zhang et al created drifting tablets of captopril utilizing HPMC (4000 and 15000 cps) and carbopol 934P. In vitro lightness concentrates on uncovered that tablets of 2 kg/cm2 hardness after drenching into the drifting media drifted right away and tablets with hardness 4 kg/cm2 sank for 3 to 4 minutes and afterward rose to the top. Tablets in the two cases stayed drifting for 24 hours.
The tablet with a hardness of 8 kg/cm2 was unable to float. It was determined that the presence of internal voids (porosity) in the tablet's center and the swelling of the hydrocolloid particles on the tablet's surface when it comes into contact with gastric fluids control the tablet's buoyancy. When compared to conventional tablets, these floating tablets had a longer release time, and the controlled release of captopril from the dosage form lasted for 24 hours.
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119 4 ADVANTAGES & DISADVANTAGE OFFLOATING DRUG DELIVERY SYSTEM 4.1 Advantages of Floating Drug Delivery System
1. When it comes to drugs that are absorbed through the stomach, the gastroretensive systems are helpful.
Such as antacids and ferrous salts.
2. When they come into contact with the stomach wall, acidic substances like aspirin irritate it. As a result, the HBS formulation might be useful for administering aspirin and other similar medications.
3. When a prolongs release floating dosage form, such as a tablet or capsule, is taken, the drug dissolves in the gastric fluid. They break down in the gastric liquid would be accessible for retention in the small digestive system after expected that a medication will be completely retained from drifting measurements structures assuming it stays in the arrangement structure even at the soluble pH of the digestive tract.
4. Drugs that are intended to have a local effect in the stomach benefit from the gastroretensive systems.
such as antacids
5. Poor absorption is to be expected when there is a rapid transit time and a vigorous intestinal movement, as in certain types of diarrhea. In such instances, it may be advantageous to keep the medication floating in the stomach for a more favorable response.
4.2 Disadvantages of Floating Drug Delivery System
1. For medications that have a problem with solubility or stability in the GI tract, a floating system is not an option.
2. In order for these systems to float and effectively coat water, the stomach must contain a significant amount of fluid.
3. Only desirable candidates are those drugs that undergo significant first-
pass metabolism and are significantly absorbed throughout the gastrointestinal tract.
4. A few medications present in the drifting framework makes disturbance gastric mucosa.
5 CONCLUSION
Due to the fact that absorption is restricted to the upper GI tract, previous studies suggest that gastro retentive drug delivery offers a number of potential benefits for drugs with low bioavailability.
Additionally, they can be delivered effectively, maximizing absorption and increasing absolute bioavailability.
Moreover, the ID of new sicknesses and the opposition displayed towards the current medications thought about the requirement for the presenting new remedial particles. As a result, a wide variety of chemical entities have been introduced that are absorbed throughout the digestive system and A specialized delivery system is required for the drugs that need to show local action in absorption sites, and FDDS has achieved this. Numerous FDDS methods, including hollow microspheres, raft forming systems, single and multiple unit HBS, and single and multiple unit gas generating systems, have been developed.
Because each of these gastroretentive drug delivery systems has distinct benefits and drawbacks, they are all intriguing and have prompted a significant amount of research and development effort. In addition, it is anticipated that additional research will be conducted in the near future, which will ultimately result in enhanced efficacy of various pharmacotherapies.
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