A Review on Novel Approach of Gastro-Retentive Oral Drug Delivery System
Anamika Saxena*, Gayatri Tiwari, Vikash Bhatt
Devsthali Vidhyapeeth College of Pharmacy, Department of Pharmaceutics, Lalpur Rudrapur Pin Code - 263148
*Corresponding Author E-mail:
ABSTRACT:
The primary goal of this review is to examine and test the efficacy of new gastroretentive techniques for dealing with drugs that are without difficulty absorbed from the gastrointestinal tract and have very short half-lives that are rapidly removed from the systemic circulation. To have an excellent therapeutic effect, these drugs must be taken frequently. A systematic search and collection of reviewed information from Pubmed, Embase, Scopus, and Scholar databases were searched from inception to identify studies on current medications. Several methods are used to retain the drug and enhancethe bioavailability, conventional effect versus floating effect. The current approaches of floating drug delivery systems can be used to reduce complex tasks associated with conventional oral dose forms and release the drug at a specific absorption site, which has been shown in these reviews to be effective in targeting drug release at a specific absorption site to improve the bioavailability of a specific drug material. Based on the data presented, the conclusion is that it can also provide local medication delivery in the stomach and proximal small intestine. To achieve the system with the intended activity, it is critical to select the right technology for the right goal via asuitable mechanism of action. These technologies can solve various problems while improving a pharmaceutical dosage form.
KEYWORDS: Floating drug delivery, Specific site release, oral drug delivery, And gastro-retentive dosage form, (GRDDS).
INTRODUCTION:
This floating drug delivery system has very low bulk density to allow any medicine to remain buoyant for up to three to four hours in the stomach with no effect on how quickly the stomach empties1. Drugs that are easily absorbed from gastrointestinal tract (GIT) and have short half-lives are eliminated quickly from the systemic circulation. Frequent dosing of these drugs is required to achieve suitable therapeutic activity. To avoid this limitation the development of oral sustained-controlled release formulations is an attempt to release the drug slowly into the gastrointestinal tract (GIT) and maintain an effective drug concentration in the systemic circulation for a long time.
Most traditional oral administration devices have demonstrated tight stomach emptying time2.
An oral controlled-release drug delivery system was used to avoid these complications, which slowly released medication into the gastrointestinal tract and maintained a constant drug absorption in the blood for an extended period.3 i.e., establishing control over gastric retention time is crucial since it enables the stomach's regulated drug release systems to remain active longer than with a typical technique. Among these challenges is maintaining the dose form in the correct gastrointestinal system position. Numerous oral administration strategies with prolonged stomach retention length have been researched to circumvent this physiological impediment.4 Any drug delivery system is to afford a therapeutic amount of drug to the proper site in the body to attain promptly, and then maintain the desired drug concentration. The plasma drug level oscillates due to the inability of the standard sustained release dosage form to extend its resistance time in the stomach and the absence of controlled drug administration. While fasting, electrical impulses occur in the stomach and intestine every two to three hours. Migratory or inter-digestive myoelectric cycles are what these are called.5
Physiology of gastroretentive tract:
The primary mechanism of the fundus of the body and the pyloric sphincterof the stomach is to store the food, grind it into pieces, and release it into the duodenum.6 The duodenum is connectedto the end of the stomach and the beginning of the intestine by the pyloric sphincter, a valve-like structurethat can open up to 12.8 mm.7 Itresulted; in larger dosage forms staying in the stomach for more extended periods. The stomach contains up to 50ml of gastric fluid at rest; in the fasting stage, the pH ranges about 1.5-2, and it increases in the fed state up to 2-6 after gastric acid is released. Gastric Content Retention In general, the duration of any particular dosage form is typically 1–2.5hours when fasted. Still, GRT is increased when fed, particularly with fat-containing foods, which aid in the passage of food from the stomach to the intestines.8
Fig.1 Physiology of stomach
Concept of gastric retention:
Numerous oral dosage forms could be employed to reduce the length of time required for an abdominal stay in the hospital by avoiding invasive procedures. There are numerous oral dosage form concepts, including a biodegradable hydrogel system, a magnetic system, a super porous system, and stomach emptying simultaneously with hunger and fullness. When you are not eating, your stomach and intestines undergo electrical processes every two to three hours. The migrating myoelectric cycle (MMC), also known as the myoelectric cycle, is divided into three phases9. The drug lasts about forty to sixty minutes except for occasional contractions in the first phase. The second phase lasts about forty to sixty minutes with intermittent activity and potential contractions. Finally, the third phase lasts up to six minutes. It consists of intense and regular contractions for a short time, resulting in the move out of all undigested materialinto the small intestine10.
Fig.2 Schematic presentation of MMC
Factors affecting the floating drug delivery system: Several factors can affect how long an oral dose stays in the stomach. The drug elements should be between 1 and 2mm in diameter to pass through the pyloric valve to the small intestine. When fasting, the stomach pH can rise to 2.0 and reach 9.0 when a considerable amount of water is consumed orally.When the drink is consumed, there is not enough time for the stomach to produce enough acid. The buoyancy of food in the stomach determines its retention, and time is a density-dependent dosage.11
Fig. 3 Factors affecting the floating drug delivery system
Size and Shape:
Those with a diameter of 7.5mm or more have more GRT than 9.9mm. According to research, tetrahedron-shaped dosage forms and ring-shaped devices have better GIT retention for 90-100 per cent at 24 hours than other shapes.12
States of Fed or Unfed:
Migrating myoelectric complexes (MMC) are bursts of intense muscular activity that occur every 1.5 to 2 hours during fasting. To expedite the unit's GRT, give the formulation with MMC, which clears the stomach of unprocessed materials.13
Nature of the meal:
Feeding indigestible polymers of fatty acid salts to the stomach can slow the gastric emptying process and prolong medication release.14
Caloric Content:
A high-protein, a high-fat meal can raise GRT for four to ten hours.15
Frequency of feed:
When a large number of meals are provided, the GRT can increase by nearly four hundred minutes due to the low frequency of MMC.
Gender/Age:
Men, regardless of their weight, height, or body surface area, had a significantly shorter mean ambulatory GRT during meals than women of comparable age and race. The elderly, particularly those over the age of 70, have significantly longer GRT.16
Posture: GRT can differ between the supine and upright ambulatory states of the patient.16
Floating drug delivery and its Advantages17,18
Floating drug delivery systems are a significant advancement in drug delivery technology since they exhibit gastric retention and offer several advantages. Increased absorption of the medicine results from the increased gastro-retentive time and the dosage form spending more time at the absorption site. In addition, biotransformation's initial pass has been enhanced. As a result, longer-lasting drug delivery and decreased dose frequency Reduced drug concentration variations, reducing mucosal irritation caused by the drug by a regulated release rate.
Fig. 4 Mechanism of floating drug delivery system
The floating medication delivery system's mechanism of action:
When it comes to creating stomach retention while maintaining acceptable bioavailability, floating drug delivery devices are one of the best options. You can use this strategy if your medication has an absorption window in the stomach or the upper small intestine.19 Since medicine has a lower density than gastric fluid, it can be administered slowly and accurately because it does not interfere with gastric emptying. Afterwards, the stomach's residual system is flushed out of the body. As a result, the stability of stomach retention and plasma medication concentrations is improved.20.
Table 1 Ideal property for developing the site-specific dosage form10,21
|
Dosage form |
Drug |
|
Microsphere |
Ibuprofen, TerfenadineTranilast, griseofulvin, Aspirin |
|
Film |
Cinnarizine, particular essential drugs, Drug delivery device |
|
Granules |
Indomethacin, prednisolone, Diclofenac sodium |
|
Tablets/pills |
Acetaminophen, Acetylsalicylic acid, Amoxicillin trihydrate, Ampicillin, Atenolol, Chlorpheniramine maleate, Diltiazem, Fluorouracil, Isosorbidedinitrate, p- Aminobenzoic acid Prednisolone, Quinidine gluconate, Riboflavin-5’-phosphate, Sotalol, Theophylline and Verapamil |
|
Capsules |
Chlordiazepoxide HCL, Propranolol HCL, Diazepam, Furosemide, L-Dopa and Benserazide, Misoprostol, Ursodeoxycholic acid |
Types of floating drug delivery systems:
Fig. 5 Classification of floating drug delivery system
Effervescent Systems:
Swellable polymers, such as methodical polysaccharides, are used to prepare these effervescent systems when they arrive in the stomach. Since CO2 is produced, the formulation can float.22
The gas generating systems:
By using effervescent reactions between carbonate and bicarbonate salts and citric or tartaric acid, these buoyant delivery systems release CO2, which lowers the specific gravity of the systems' jellified hydrocolloid layer and allows the delivery systems to float above the contents of the stomach.23.
Volatile liquid system:
To fill the stomach chamber at body temperature, a gasified volatile liquid, such as ether or cyclopentane, is used in the floating drug. The device can expand and float above the stomach secretions through an inflatable chamber that vaporizes at body temperature24.
Intragastric floating drug deliverysystem:
This system is comprised of a floating chamber containing a vacuum or an inert, harmless gas, as well as a microporous compartment housing a drug reservoir.25
Inflatable gastric floating drug delivery system:
The design incorporates an inflatable chamber containing liquid ether, which gasifies when heated by the body and inflates the stomach chamber. A drug reservoir, either a drug or a polymeric matrix impregnated with a drug, is filled into an inflated chamber and sealed with a gelatin capsule to create these devices. The capsule melts after oral administration, releasing the drug reservoir and expanding the stomach's self-inflating pharmacological reservoir compartment. The reservoir delivers medication to the digestive system continuously.3
Non-effervescent systems:
Floating drugs are administered based on the swelling or adhesion of the polymer to the GIT mucosa. Excipients such as polysaccharides, hydrocolloids, polyacrylates and polycarbonates, carbopol and bioadhesive polymers like carbopol and chitosan are the most common in non-effervescent FDDS. When they contact stomach fluid, gel-forming hydrocolloids expand, but they retain their relative shape integrity and a bulk density lower than unity.26
Raft forming system:
An alginate solution (sodium alginate, calcium carbonate, or bicarbonate) creates a thick cohesive gel with trapped CO2 bubbles in the gastric fluid, allowing medication to be slowly delivered into the stomach when these systems come into contact with it. Ulcers and gastroesophageal reflux disease are two common conditions for using these devices.27
Fig.7 (A) conventional effect (B) floating effect drug absorption window
Colloidal Gel Barrier System:
Because gel-forming hydrocolloids prolong the gastro-retentive period and increase the amount of medicine taken at the absorption site, they are referred to as a hydrodynamically balanced system. This method employs gel-forming substances such as hydroxyl-ethyl cellulose, polysaccharides, hydroxymethyl cellulose, hydroxypropyl cellulose and matrix-forming polystyreneand polycarbophil.22.
Fig. 8 Schematic diagram of formation of alginate beads
Calcium alginate, freeze-dried, was used to create the multi-unit floating dosage forms. When a sodium alginate solution is dropped into an aqueous calcium carbonate solution, the calcium alginate precipitates.A porous system with a floating force of roughly 12 hours forms, resulting in spherical beads with a diameter of about 2.5mm. The resident length of these floating beads was longer than that of solid beads, which had a one-hour residence period28.
Bilayer floating tablet:
Two layers of immediate-release tablets deliver the initial dose to the system, while the sustained-release layer absorbs stomach fluid and forms a colloidal gel barrier on the surface. It will float in the stomach due to its mass density being less than one.
Micro-porous compartment system:
This method employs drug reservoir encapsulation technology, including perforations on a microporous compartment's top and bottom walls. The drug reservoir compartment's peripheral wall is sealed to prevent undissolved medications from contacting the stomach surface. Because of the entrapped air in the floating chamber, the delivery system floats above the gastric contents of the stomach. Gastric fluid flows through the aperture, obstructing pharmacological activity and transferring dissolved drugs across the gut for absorption29,30.
Microspheres/hollow micro balloons:
The plasticizer polymer ratio and solvent were added to a 40°C agitated solution of poly Vinyl Alcohol to increase the dosage form's stomach retention time via simple solvent evaporation buoyancy. The more polymers in the dosage form, the greater the release of the drug. In drug manufacturing, dichloromethane is synthesized within the polymer and evaporates from the droplet's gas phase31.
Fig.9 schematic representation of micro-balloon and hollow sphere
Evaluation parameter of floating drug delivery system:
Surface characterization:
Drug solubility and bioavailability are greatly affected by the particle size and shape. All of these techniques, as well as optical microscopes, ultrasound attenuation spectroscopy and a variety of sedimentation methods and electro resistance counting, photo analysis and laser diffraction methods and measurements of air pollution emissions, are used to figure out the formulation's particle size32.
Swelling studies:
Temperatures were maintained at 37.0.5°C while the tablet was placed in the glass beaker and dissolved in the water bath. Regularly, the tablet was removed, and filter paper was used to remove the excess fluids from the surface. They were recalculating the massive pill's weight (W2). The previously published Formula was used to calculate the Swelling Index (S.I.)33.
S.I. = W2 – W1 / W1
Floating lag time:
The experiment recorded floating time using a USP dissolving apparatus-II at 50 RPM with 900ml of 0.1N HCl and a temperature of 37 0.5oC. In addition, visual inspection is used to evaluate how long the tablet floats in the dissolving liquid34.
Drug content:
Temperatures were maintained at 37.0.5°C while the tablet was placed in the glass beaker and dissolved in the water bath. Regularly, the tablet was removed, and filter paper was used to remove the excess fluids from the surface. They were recalculating the massive pill's weight (W2). The previously published Formula was used to calculate the Swelling Index (S.I.)35.
Determination of viscosity:
The viscosity of each gel sample was measured at room temperature using a Brookfield digital viscometer coupled with a spindle number at shear rates ranging from 10 to 100RPM.
Resultant/Weight test:
The equipment was designed to evaluate the true floating capability of buoyant dosage forms over time. It works by computing the force equivalents of the forces needed to keep the object submerged in the fluid.
B. For Multiple Unit Dosage Forms:
Entrapment efficiency:
A suitable process is used to extract, examine, and compute the drug. Efficacy of drug entrapment =Amount of drug supplied /Theoretical drug-loaded expected*10036.
Buoyancy or Floating test:
It is measured how long it takes for the dosage form to become buoyant and how long it remains buoyant after administration in simulated stomach fluid. It is important to note that the dosage form's buoyancy lag time, or floating lag time, is the time it takes for the dosage form to emerge from a medium.37
Swelling study:
Its weight gain or water consumption determines a dosage form's swelling behaviour. The growth in tablet diameter and thickness over time could be used to quantify the dimensional changes. The equation can compute water uptake as a percentage of weight gain.32
In vitro floating ability (Buoyancy %):
As many as microspheres as can be counted are evenly dispersed over the surface of a USP (Type II) dissolution device which has been pre-mixed for 12 hours at 100 revolutions per minute (rpm) with 900 millilitres (0.1% NHCl) and 0.02 percent (v/v) Tween 80. After 12 hours, the settling and floating layers are removed, desiccated, and weighed.38
Buoyancy (%) = Wf / (Wf + Ws) * 100
In-Vivo Method:
X-Ray technique X-ray technologies are now frequently utilized to assess floating drug delivery systems. It aids in establishing the position of a dosage form in the G.I. tract and the relationship between stomach emptying time and dosage form passage through the gastrointestinal tract.39
Gastroscopy:
A fibre optic and video system are utilized in conjunction with peroral endoscopy. The effect of prolonged exposure to the gut environment on the floating medicine delivery system may be visualized via gastroscopy.39
Ultrasonography:
Ultrasound waves reflected acoustic impedances that varied considerably across the interface, allowing imaging of several abdominal organs. Most D.F.s exhibited no significant auditory differences during contact with the physiological milieu. The findings will be displayed as still photos or a video of the inside of the body. As a result, this method is rarely used to assess Floating Type Drug Delivery Systems.40
Stability study:
The ultrasound waves reflected acoustic impedances that varied widely across the interface, allowing imaging of many abdominal organs. During their encounter with the physiological milieu, most D.F.s showed no significant hearing abnormalities. The findings will be shown in the form of still photos or a movie of the inside of the body. As a result, Floating Type Drug Delivery Systems are rarely evaluated using this method.41
Floating drug delivery system application:
Enhanced bioavailability:
Riboflavin CR-GRDF is significantly more bioavailable than non-GRDF controlled release polymeric formulations. There are multiple mechanisms involved in medicine absorption and transit through the G.I. Tract.42.
Table: 2 Comparison between Conventional drug delivery systems and GRDDS
|
S.No |
Drug |
Class |
Conventional effect |
Floating effect |
|
1 |
Atenolol |
Beta-blocker |
Conventional dosage forms of Atenolol have been poorly absorbed from the lower label of the gastrointestinal tract. |
Floating in vitro drug release tests revealed that Atenolol bioavailability was improved, and drug release was extended (99.5 percent) for 24 hours. In addition, it increases the stomach residence time by following zero-order kinetics48. |
|
2 |
Azelnidipine |
Dihydropyridine calcium channel blocker |
Azelnidipine has a lower bioavailability during when fasting stage because it is practically soluble in water and gut area and metabolized in cytochrome p450. |
However, Azelnidipine floating tablets were formulated as gas-producing agents, which increased G.I. transit time and improved bioavailability49. |
|
3 |
Captopril |
ACE inhibitor |
Captopril is subjected to the first Pass effect and having low half life50. |
Captopril provided extended-releaseand improved mechanical strength of the tablet, which maintained its sustained drug delivery release formulation51. |
|
4 |
Cephalexin |
Cephalosporin antibiotics |
Cephalexin hasrapid hydrolysis and de-esterification Because esterase enzymes' intestinal mucosa penetration is minimized52. |
Floating drug delivery systems formulated and improved drug bioavailability, significantly reducing enzymatic degradation and minimizing dose dumping53. |
|
5 |
Cefodoxime Proxetil |
Cephalosporin antibiotics |
Cefpodoxime has degradation chances in GIT, and also Elimination half-life is reduced54. |
Cefpodoximeproxetil locust bean gum is a superior option for controlled release action. In addition, bioavailability has improved, as has the floating lag time55. |
|
6 |
Clarithromycin |
Macrolide antibiotic |
Drug resistance is caused by a short stomach residence period and the necessity for a high drug concentration 56. |
Clarithromycin-loaded gastroretentive tablets have swelling qualities developed to extend the time the antibiotic stayed in the stomach57. |
|
7 |
Glipizide |
Anti-diabetic |
conventional strategies of prolonging the release of the dosage forms throughout the GIT would not be an effective formulation as it is mainly absorbed starting in the small intestine58. |
Glipizide gastro-retentive dosages improve the medicine's solubility and are designed to regulate and complete drug release for an extended period59. |
|
8 |
Hydralazine |
Vasodilators |
Hydralazine synthesis and preparation Compared to formulations with a lower concentration of polymers, polymer concentration resulted in slower drug release. 60. |
With HPMC present, a prolonged-release pattern with a good swelling index and a floating effect improves drug absorption due to increased gastro-retentive time.61. |
|
9 |
Omeprazole |
Proton pump inhibitor |
Omeprazole has degraded in the acidic medium breakdown, making conversion more complex 62. |
Omeprazole drug was protected throughout the GIT, its solubility in the intestine was improved, and its permeability and drug release adjustment63. |
|
10 |
Ritonavir |
Protease-inhibitor |
Ritonavir Due to an intractable problem, oral bioavailability has been lowered. As a result, gives solubility is poor 64. |
Ritonavir in a gastro-retentive dose form improved the drug's oral bioavailability. And minimized the side effect65. |
|
11 |
Ranitidine hydrochloride |
H2-receptor antagonist |
Ranitidine hydrochloride hasa poor half-life of 2–3 hours, absorption diminishes from the upper GIT to the colon, and is vulnerable to microbial destruction; a high dose frequency is required66. |
Ranitidine hydrochlorideprovided increased floating time in the stomach, thus improving gastric retention and reducing the process of dose dumping 67. |
|
12 |
Simvastatin |
HMG-CoA reductase inhibitor |
Simvastatin has a short half-life and limited absorption in the lower gastrointestinal system68. |
The articles conclude that First-pass biotransformation is improvedand floated on the test medium for additional12 hours 9-minute floating lag time. As a result, the occurrence of HPMC 69. |
|
13. |
Pregabalin |
Anticonvulsant |
The pregabalinclass 1 drug hasa short half-life, is absorbed in the upper gastrointestinal tract and requires a high dose frequency70. |
According to this study, Pregabalin reduced drug concentration variations and decreased mucosal irritation produced by medicines released slowly and at a controlled rate71. |
Sustain-release drug delivery:
Oral C.R. formulations have been associated with problems with gastric residence time in the G.I. tract. HBS systems can avoid these concerns by utilizing chemicals with a high enough bulk density to float on top of gastric fluids and stay in the stomach for a long time. These are larger devices that are not authorized to enter the pyloric opening.43.
Site-specific drug delivery system:
Patients with stomach or near-small-intestinal absorption of medication can benefit from these methods. Regulated and gradual dosing ensures that the patient receives enough local therapeutic doses while minimizing systemic exposure to the drug. The prolonged gastrointestinal availability of a site-guided delivery device can reduce dosing frequency. Examples include furosemide and riboflavin.44.
Absorption Enhancement:
Because site-specific absorption for the upper gastrointestinal tract is potentially used for a floating drug delivery system, these drugs have poor bioavailability.45.
Reduced Adverse Colon Activity:
The amount of medication that enters the colon is reduced when drugs are retained in the stomach's HBS systems. As a result, the medicine's colon-damaging effects could be avoided. The pharmacodynamics component is justified by using GRDF formulations for beta-lactam antibiotics, which are only absorbed in the small intestine and whose presence in the colon results in microorganism resistance.45.
Reduced fluctuations in the concentration of the drug:
When CRGRDF is administered via continuous infusion rather than immediate-release dose formulations, drug concentrations in the blood are more stable. As a result, medication volatility is reduced, and concentration-dependent adverse effects are avoided. This is especially true for medications with a narrow therapeutic range.46
Maximize the bioavailability:
The drug's duration of action A gastro-retentive delivery mechanism is utilized to prolong the doses' activity to improve absorption.47
CONCLUSION:
Drugs having short half-lives and easy absorption from the gastrointestinal tract (GIT) can be quickly removed from systemic circulation using a gastro-retentive drug delivery device. These medications must be used regularly to have the desired therapeutic effect. This review emphasized the conventional and floating effect technologies that have evolved to overcome this limitation, exposing various methods for keeping the medication in the G.I. area for more extended periods while raising drug concentrations in the systemic circulation. Oral sustained-release formulations gently release the medication into the digestive tract while keeping an effective drug concentration in the systemic circulation.
An effective floating drug delivery system, which has been a simple job for many medications in the preceding decade, has permitted higher bioavailability and regulated dispersion of many pharmaceuticals, resulting in new and improved treatment options. However, many issues must be addressed to maintain gastric retention for an extended period. Therefore, many pharmaceutical companies have prioritized the commercialization of this Formula. Gastrointestinal movement time control using advanced technologies such as conventional pill endoscopy is the mainstay of novel therapy choices with great patient benefits.
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Received on 08.07.2022 Modified on 10.10.2022
Accepted on 13.12.2022 ©Asian Pharma Press All Right Reserved
Asian J. Res. Pharm. Sci. 2023; 13(2):145-153.
DOI: 10.52711/2231-5659.2023.00026