International Journal of Advanced Science and Technology Vol. 29, No. 5, (2020), pp. 3613 - 3627 Recent Advances in the Development of Floating Microspheres for the Treatment of Gastric Ulcers Radha Rani1, Manish Kumar*1, Narendra Yadav2, Shailendra Bhatt1, Anuj Malik1, Beena Kumari3, Sangeeta3, Dilshad4, Anil Kumar5 1MM College of Pharmacy, Maharishi Markandeshwar (Deemed to be University) Mullana, Ambala, India 2Rajiv Academy for Pharmacy, Mathura, UP, India 3Department of Pharmaceutical Sciences, Indira Gandhi University, Meerpur, Rewari, Haryana, India 4DVM College of Pharmacy, Sohna, Haryana 5Guru Jambheswar University of Science and Technology, Hisar, Haryana, India *ˡ [email protected], Abstract Ulcers are lesions which is a discontinuity of gastrointestinal mucosa. A variety of medications are used to treat mild to reasonable ulcers. Drugs used to treat ulcers are called anti-ulcer drugs. Floating microspheres organized by solvent-evaporation method using polymers and solvents whose particle size analysis, encapsulation efficiency, scanning electron microscopy and drug loading, in-vitro release study, stability studies characterization was carried out which showed an better absorption and bioavailability by retaining the system in abdomen for a extended period of time. Large efforts have been made global to investigate these systems rendering to patient necessities, both in terms of compliance and therapeutic efficacy. Floating microspheres as gastro retentive dosage forms exactly manage the release rate of target drug to a particular site and enable a vast impact on physical condition. This review in brief 87klj emphasizes on Gastro Retentive Drug Delivery system of anti-ulcer drug. Special categories parallel to antacids, anti diabetic, antifungal and anticancer drugs are formulated into Floating. Drug Delivery System. These systems also present fabulous openings in the designing of most recent controlled and delayed release oral formulations, thus extending the frontier of futuristic pharmaceutical enlargement. In the present review advantages, preparation methods and applications are discussed. Keywords: Floating microspheres, Solvent evaporation method, Ulcers. 1. Introduction In these days traditional drug delivery methods are the elementary pharmaceutical products generally seen in formulas and over the counter marketplace. They endow a fast release of drug but in order to get and presence the concentration too within the therapeutically cognizable range [1, 2]. It is frequently essential to given it many times a day, out coming in valued up and downs drug grades. Even if these jobbers are formulated so as to yield utmost fixity, activity and bioavailability, some drugs are unsteady or virus and have limited therapeutic quantity of drug to the reasonable point in the body to take neon and then maintain the required drug concentration. This ideal goal is indicative of most prominent two aspects of drug delivery local location and temporal delivery of a drug, spatial location concerning targeting a drug for a particular part or a tissue. While short dated delivery stands for restraining the price of drug delivery that distinct organ or tissue [3-6]. Controlled drug release technique expresses one of the border areas of knowledge, which implicates multidisciplinary scientific outlook. Contributing to kindly health caution. ISSN: 2005-4238 IJAST 3613 Copyright ⓒ 2020 SERSC International Journal of Advanced Science and Technology Vol. 29, No. 5, (2020), pp. 3613 - 3627 These drug delivery systems have a great possible of resolving the puzzles communicated with the traditional various dosing mode like strict obedience to periodic dosing. Flip flop plasma concentration, concomitant side impacts on account of systemic congregation of drug and non-compliance of patient. Hence, there are many profits such as improved impression reduced venomousness improved patient compliance and facility etc [7, 8]. In spite of partial release of the drug and a less swelling time of dosage forms in the upper gastrointestinal method, a major spot for soaking of many drugs will guide to short bioavailability. Attempts to repair verbal drug bioavailability have grown in equal with the pharmaceutical vocation. As the figure and chemical variety of drugs has enhanced, new strategies are needed to cultivate verbally deadfall therapeutics. The past two dickers have been marked out by an enhanced understanding of the reason of law bioavailability and a mighty bargain of nicely of oral delivery techniques spotted by unique growth of the drug delivery industry. Therefore belly ache retentive dosage forms which increase the habitation time of the drugs in the stomach and renovate them bioavailability have been elevated [9]. Targeting delivery of drugs to sick wounds is one of the most prominent facts of drug delivery systems. To cost an enough dose of drug to the lesion, appropriate bearers of drugs are demanded. Nano and very thin particulate carriers have major consumptions for administrations of therapeutic particle. Investigation in the regions is being carried out all over the world at a great motion. Peerless sophisticated systems are now being elevated with the purpose of targeting drugs to exclusive body spot and hindering the proportion of drug delivery of drugs to target spots hence increasing the capacity of drug delivery [10, 11]. 2. Peptic Ulcer Peptic ulcer constitutes a large scale problem in hyperacidity patients, which is due to infection of stomach or duodenal mucosal lining of the GIT. In the any part of the GIT peptic ulcer occurs which is discovered to pepsin and gastric acid i.e. the duodenum and stomach [12]. Generally acid secretion is nature in gastric ulcer. Acid secretion is large in divided of the patients in duodenal ulcer but normal in the rest. Acid build-up are either normal or even high, though it contributes to the ulcers, an invasive component whose contraction is the main method of ulcers treatment. An understanding of regulation of acid secretion and the mechanism will elucidate the targets of anti-secretory action as shown in Fig. 1 [13-15]. Figure 1. Peptic Ulcer 2.1 Pathogenesis of Peptic Ulcer ISSN: 2005-4238 IJAST 3614 Copyright ⓒ 2020 SERSC International Journal of Advanced Science and Technology Vol. 29, No. 5, (2020), pp. 3613 - 3627 By H. pylori approximately half population of the world’s is colonized, which ruins most important reason of peptic ulcers [16]. In developing countries, the occurrence of H. pylori is higher, especially in Central Asia, Africa, Eastern Europe and Central America [17]. In a free and crowded environment, this organism is cultivated in childhood and in countries where the socioeconomic conditions are low. By H. pylori epithelial cell degeneration and injury caused which is usually more severe in the antrum, by plasma cells, neutrophils, macrophages and lymphocytes accompanied by inflammatory response. The mechanism of development of various types of lesions induced by H. pylori in the gastro duodenal mucosa has not been fully explained. H. pylori infection can outcome in hyper chlorhydria. The main mediators of H. pylori infection is the cytokines that inhibit parietal cell secretion, but the activate calcitonin gene-related peptide (CGRP) can directly affected by H.pylori, sensory neurons are linked with somatostatin, H+/K+ ATPase α-subunit, and the production of gastric inhibited[18]. Different classes of drugs their mechanism of action with adverse effects are listed in table 1 [19-31] and Therapy combination type and efficiency of Helicobacter pylori elimination treatment options are listed in table 2 [32-37]. Table 1. Mechanisms of action and adverse effects of the most commonly used Anti-ulcer treatment option Class of Medicine Mechanism of Adverse effect Reference Drugs action Proton Omeprazole Inhibition of Abdominal pain 32,33 pump Lansoprazole the gastric Diarrhea Nausea inhibitor Rabeprazole H+/K+- Vomiting Esomeprazole ATPase Constipation Pantaprazole (proton pump) Flatulence enzyme Vitamin B12 system deficiency Osteoporosis H2 Cimetidine Blocking the Headache Anxiety 34 Receptor Famotidine action of Depression Blockers Nizatidine histamine at Dizziness Ranitidine the histamine Cardiovascular H2 receptors events of parietal Thrombocytopenia cells Antacids Aluminum Increases Frequency not 35 hydroxide gastric pH to defined: Nausea Magnesium greater than Vomiting Hypo hydroxide four, and phosphatemia inhibits the Chalky taste proteolytic Constipation activity of Abdominal pepsin causes cramping Diarrhea osmotic Electrolyte retention fluid imbalance Potassium- Vonoprazan Inhibits H+, Nasopharyngitis 36-42 Competitive Misoprostol K+-ATPase in Fall Contusion Acid Sucralfate gastric parietal Diarrhea Upper Blocker cells at the respiratory tract ISSN: 2005-4238 IJAST 3615 Copyright ⓒ 2020 SERSC International Journal of Advanced Science and Technology Vol. 29, No. 5, (2020), pp. 3613 - 3627 cyto final stage of inflammation protective the acid Eczema Agents secretory Constipation Back pathway pain Stimulate Diarrhea mucus Abdominal pain production and Headache enhance blood Constipation flow throughout the lining of the gastrointestinal tract Table 2. Types and efficiency of Helicobacter pylori (H. pylori) eradication treatment options Type Duration Efficiency Reference First line Standard triple therapy: 7–14 days 70-85 % 43 PPI + two antibiotics (clarithromycin + metronidazole or amoxicillin Second line Bismuth- containing quadruple therapy: 14 days 77-93%