The aim of the present study was to prepare and evaluate a novel buccal adhesive system (NBAS) containing propranolol hydrochloride (PH). A special punch was fabricated and used while preparing an NBAS. Solubility of PH in phosphate buffer solution (pH 6.6), partition coefficient between phosphate buffer (pH 6.6) and 1-octanol, and permeability coefficient through the porcine buccal mucosa were performed and found to be 74.66 mg/mL, 5.17, and 5.6, respectively. Stability of NBAS was determined in natural human saliva, and it was found that both PH and device are stable in human saliva. NBAS was evaluated by weight uniformity, thickness, hardness, friability, swelling, mucoadhesive strength, in vitro drug release, and in vivo human acceptability studies. Swelling index was higher (4.4) for formulations containing hydroxyl propyl methyl cellulose (HPMC) K4M alone, and it decreases with its decreasing concentration in the NBAS. Mucoadhesive strength (MS) was measured by using a modified apparatus. All NBASs showed higher MS with porcine buccal mucosa when compared with that of rabbit buccal mucosa. NBASs containing carbopol (CP) 934P and HPMC K4M at the ratio of 1:1 showed higher MS (44.76 g) with porcine buccal mucosa when compared with 1:2 (39.76 g), 0:1 (23.29 g), and 1:0 (22.22 g) ratios, respectively. The mechanism of PH release was found to be by non-Fickian diffusion (value of "n" between 0.5 and 1.0) and followed first order kinetics. In vivo human acceptability study showed that the newly prepared NBAS was comfortable in the human buccal cavity. It can be concluded that NBAS is a superior, novel system that overcomes the drawback associated with the conventional buccal adhesive tablet.KEYWORDS: buccal delivery, carbopol 934P, HPMC K4M, propranolol hydrochloride, mucoadhesion. INTRODUCTIONIn recent years, delivery of therapeutic agents through various transmucosal routes has gained significant attention owing to their presystemic metabolism or instability in the acidic environment associated with oral administration. [1][2][3][4][5] The oral mucosa can be categorized into sublingual, gingival, and buccal mucosa through which oral transmucosal delivery can be achieved. Absorption of therapeutic agents from the oral cavity provides a direct entry of such agents into the systemic circulation, thereby avoiding the first-pass hepatic metabolism and gastrointestinal degradation. 6-8 However, the buccal route of drug delivery has received much more attention because of its unique advantages over other oral transmucosal routes. 7,[9][10] Delivery of various therapeutic agents via the buccal route using conventional matrix tablets, films, bilayered systems, and hydrogel systems has been studied and reported by several research groups. 11-16 A number of formulation and processing factors can influence properties and release properties of the buccal adhesive system. The conventional buccal adhesive tablets have some limitations: (1) conventional tablets may not have a uniform adhesive layer, leading to weak ad...
Arthritis refers to different medical conditions associated with disorders of the primary structures that determine joint functioning, such as bones, cartilage, and synovial membranes. Drug discovery and delivery to retard the degeneration of joint tissues are challenging. Current treatment of different types of arthritis such as osteoarthritis, rheumatoid arthritis, septic arthritis, juvenile idiopathic arthritis, and ankylosing spondylitis involves the administration of nonsteroidal anti-inflammatory drugs (NSAIDs) such as aspirin, diclofenac, aceclofenac, ibuprofen, flurbiprofen, indomethacin piroxicam, dexibuprofen, ketoprofen, nabumetone, nimesulide, and naproxen, mainly by the oral, parenteral, or topical route. However, the frequent dosing that is required with NSAIDs often leads to patient noncompliance, so drug-delivery technologies should be developed to reduce the frequency of dosing and to allow sustained release of medications. Microencapsulation is one of the novel drug-delivery technologies employed to sustain drug release. This method reduces dosing and eliminates gastrointestinal irritation, thus ultimately improving patient compliance in the pharmacotherapy of arthritis. We provide a comprehensive overview of several microencapsulation technologies used in the treatment of arthritis that may reduce the dose-related adverse effects caused by NSAIDs.
Rheumatoid arthritis (RA) is a painful, debilitating disease characterized by inflammation of the joints, with the proliferation of the synovium and the progressive erosion of cartilage and bone. The treatment of RA is still unsatisfactory, but a number of powerful disease-modifying antirheumatic drugs have become available, such as methotrexate (MTX). Even in the current era of biological targeted therapies, MTX remains the initial preferred antirheumatic drug and is considered to be the gold standard for treatment of RA. The combination of its perceived efficacy, acceptable safety profile, and low cost, as well as decades of clinical experience, makes MTX the cornerstone of treatment for RA and the anchor drug in combination with various biological agents. In this review, the authors aim to summarize the research done in the field of drug delivery systems of MTX according to its routes of administration for treatment of RA. The last part of the review addresses combination therapy with MTX and future direction in the drug delivery of MTX. This review also provides the reader with a general overview of RA and its therapeutic strategies with respect of MTX, which may bring uniformity in medical practice for effective management of RA.
A novel colon targeted tablet formulation was developed using natural polysaccharides such as chitosan and guar gum as carriers and diltiazem hydrochloride as model drug. The prepared blend of polymer-drug tablets were coated with two layers, inulin as an inner coat followed by shellac as outer coat and were evaluated for properties such as average weight, hardness and coat thickness. In vitro release studies of prepared tablets were carried out for 2 h in pH 1.2 HCl buffer, 3 h in pH 7.4 phosphate buffer and 6 h in simulated colonic fluid (SCF) in order to mimic the conditions from mouth to colon. It was observed that 4% w/v of rat cecal contents in saline phosphate buffer (SCF) incubated for 24 h provides suitable conditions for in vitro evaluation of the formulations prepared. The drug release from the coated system was monitored using UV/ Visible spectroscopy. In vitro studies revealed that the tablets coated with inulin and shellac have controlled the drug release in stomach and small intestinal environment and released maximum amount of drug in the colonic environment. Among the polymers used, chitosan was found to be the suitable polymer for colon targeting. The study revealed that polysaccharides as carriers and inulin and shellac as coating materials can be used effectively for colon targeting of drugs for treating local as well as systemic disorders.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.