Mucoadhesive Buccal Drug Delivery System: a Review
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Novel Mucoadhesive Polymers –A Review Received On: 05-10-2011 Revised On: 13:10:2011 Accepted On: 22-10-2011
Journal of Applied Pharmaceutical Science 01 (08); 2011: 37-42 ISSN: 2231-3354 Novel Mucoadhesive Polymers –A Review Received on: 05-10-2011 Revised on: 13:10:2011 Accepted on: 22-10-2011 Mythri .G, K. Kavitha, M. Rupesh Kumar, Sd. Jagadeesh Singh ABSTRACT The current article focuses on polymers used in mucosal delivery of therapeutic agents. The mucoadhesive drug delivery system is a popular novel drug delivery method because mucous membranes are relatively permeable, allowing for the rapid uptake of a drug into the systemic circulation and avoiding the first pass metabolism. Mucoadhesive polymers have been utilized in many different dosage forms in efforts to achieve systemic delivery of drugs through the different mucosa. These dosage forms include tablets, patches, tapes, films, semisolids and powders. The Mythri .G, K. Kavitha, M. Rupesh objective of this review is to study about novel mucoadhesive polymers and to design improved Kumar, Sd. Jagadeesh Singh drug delivery systems. Department of Pharmaceutics, East Point College of Pharmacy, Bangalore, India Keywords: Novel drug delivery system; mucoadhesion; mucoadhesive polymers. INTRODUCTION The focus of pharmaceutical research is being steadily shifted from the development of new chemical entities to the development of novel drug delivery system (NDDS) of existing drug molecule to maximize their effective in terms of therapeutic action and patent protection (Berressem, 1999, Das, 2000). The development of NDDS has been made possible by the various compatible polymers to modify the release pattern of drug. In the recent years the interest is growing to develop a drug delivery system with the use of a mucoadhesive polymer that will attach to related tissue or to the surface coating of the tissue for the targeting various absorptive mucosa such as ocular, nasal, pulmonary, buccal, vaginal etc. -
Preparation of Mucoadhesive Patches for Buccal Administration of Metoprolol Succinate: in Vitro and in Vivo Drug Release and Bioadhesion
Verma & Chattopadhyay Tropical Journal of Pharmaceutical Research February 2012; 11 (1): 9-17 © Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, 300001 Nigeria. All rights reserved . Available online at http://www.tjpr.org http://dx.doi.org/10.4314/tjpr.v11i1.2 Research Article Preparation of Mucoadhesive Patches for Buccal Administration of Metoprolol Succinate: In Vitro and In Vivo Drug Release and Bioadhesion Navneet Verma 1,2* and Pronobesh Chattopadhyay 3 1College of Pharmacy, IFTM University, Moradabad-244001 (U.P.), 2Institute of Pharmacy, Bhagwant University, Ajmer-305004 (Raj.), 3Defence Research Laboratory, Tejpur-784001 (Assam), India Abstract Purpose: To develop mucoadhesive patches for buccal administration of metoprolol succinate and to evaluate their in vitro and in vivo bioadhesion. Methods: The mucoadhesive buccal patches were prepared by solvent casting technique using two different mucoadhesive polymers. The formulations were tested for in vitro drug permeation studies, buccal absorption, in vitro drug release studies, moisture absorption as well as for in vitro and in vivo bioadhesion. Results: The peak detachment force and work of adhesion for MC5 (sodium carboxymethylcellulose, i.e., Na CMC) patch were 0.87 N and 0.451 mJ respectively and the corresponding values for CH5 (chitosan) were 5.15N and 0.987 mJ. Formulation CH5 (prepared with chitosan) showed 67.1 % release, while MC5 (Na CMC) showed drug release of 81.9 % in 6 h. Basic pharmacokinetic parameters such as C max , T max and AUC total varied statistically (p < 0.05) when given by the buccal route compared with that of the solution given by the oral route. -
An Overview On: Sublingual Route for Systemic Drug Delivery
International Journal of Research in Pharmaceutical and Biomedical Sciences ISSN: 2229-3701 __________________________________________Review Article An Overview on: Sublingual Route for Systemic Drug Delivery K. Patel Nibha1 and SS. Pancholi2* 1Department of Pharmaceutics, BITS Institute of Pharmacy, Gujarat Technological university, Varnama, Vadodara, Gujarat, India 2BITS Institute of Pharmacy, Gujarat Technological University, Varnama, Vadodara, Gujarat, India. __________________________________________________________________________________ ABSTRACT Oral mucosal drug delivery is an alternative and promising method of systemic drug delivery which offers several advantages. Sublingual literally meaning is ''under the tongue'', administrating substance via mouth in such a way that the substance is rapidly absorbed via blood vessels under tongue. Sublingual route offers advantages such as bypasses hepatic first pass metabolic process which gives better bioavailability, rapid onset of action, patient compliance , self-medicated. Dysphagia (difficulty in swallowing) is common among in all ages of people and more in pediatric, geriatric, psychiatric patients. In terms of permeability, sublingual area of oral cavity is more permeable than buccal area which is in turn is more permeable than palatal area. Different techniques are used to formulate the sublingual dosage forms. Sublingual drug administration is applied in field of cardiovascular drugs, steroids, enzymes and some barbiturates. This review highlights advantages, disadvantages, different sublingual formulation such as tablets and films, evaluation. Key Words: Sublingual delivery, techniques, improved bioavailability, evaluation. INTRODUCTION and direct access to systemic circulation, the oral Drugs have been applied to the mucosa for topical mucosal route is suitable for drugs, which are application for many years. However, recently susceptible to acid hydrolysis in the stomach or there has been interest in exploiting the oral cavity which are extensively metabolized in the liver. -
Buccal Tablets
HIGHLIGHTS OF PRESCRIBING INFORMATION • As a part of the TIRF REMS Access program, fentanyl buccal tablets These highlights do not include all the information needed to use fentanyl may be dispensed only to patients enrolled in the TIRF REMS Access buccal tablets safely and effectively. See full prescribing information for program. For inpatient administration of fentanyl buccal tablets (e.g., fentanyl buccal tablets. hospitals, hospices, and long-term care facilities that prescribe for inpatient use), patient and prescriber enrollment is not required. Fentanyl Buccal Tablets, CII ----------------------DOSAGE AND ADMINISTRATION---------------------- Initial U.S. Approval: 1968 • Patients must require and use around-the-clock opioids when taking WARNING: LIFE-THREATENING RESPIRATORY DEPRESSION; fentanyl buccal tablets. (1) ACCIDENTAL INGESTION; RISKS FROM CYTOCHROME P450 • Use the lowest effective dosage for the shortest duration consistent with 3A4 INTERACTION; RISKS FROM CONCOMITANT USE WITH individual patient treatment goals. (2.1) BENZODIAZEPINES OR OTHER CNS DEPRESSANTS; RISK OF • Individualize dosing based on the severity of pain, patient response, prior MEDICATION ERRORS; ADDICTION, ABUSE, AND MISUSE; analgesic experience, and risk factors for addiction, abuse, and misuse. REMS; and NEONATAL OPIOID WITHDRAWAL SYNDROME (2.1) See full prescribing information for complete boxed warning. • Initial dose of fentanyl buccal tablets: 100 mcg. (2.2) • Serious, life-threatening, and/or fatal respiratory depression has • Initiate titration using multiples of 100 mcg fentanyl buccal tablets. Limit occurred. Monitor closely, especially upon initiation or following a patient access to only one strength of fentanyl buccal tablets at any one dose increase. Due to the risk of fatal respiratory depression, fentanyl time. (2.3) buccal tablets are contraindicated in opioid non-tolerant patients (1) • Individually titrate to a tolerable dose that provides adequate analgesia and in management of acute or postoperative pain, including using single fentanyl buccal tablets. -
Buccal Administration of Estrogens
Europaisches Patentamt European Patent Office GO Publication number: 0 286 581 Office europeen des brevets A1 EUROPEAN PATENT APPLICATION Application number: 88730081.2 mt. a.*: A 61 K 31/565 A 61 K 47/00, A 61 K 9/20 Date of filing: 08.04.88 Priority: 10.04.87 US 37273 @ Applicant: ZETACHRON, INC. Post Office Box 339, 100 North Science Park Road Date of publication of application: State College, PA 16803 (US) 12.10.88 Bulletin 88/41 @ Inventor: Keith, Alec D. Designated Contracting States: 539 Beaumont Drive AT BE CH DE ES FR GB GR IT LI LU NL SE Boalsburg Pennsylvania 16801 (US) Snipes, Wallace C. Deepwood Drive Pine Grove Mills Pennsylvania 16868 (US) @ Representative: UEXKULL & STOLBERG Patentanwalte Beselerstrasse 4 D-2000 Hamburg 52 (DE) @ Buccal administration of estrogens. (g) An adequate blood plasma level of 17-beta-estradiol or ethinyl estradiol is attained in a patient in need of estrogen therapy by administration of a dose of 17-beta-estradiol or ethinyl estradiol or a pharmaceutically acceptable ester thereof not greater than 1 50 micrograms into the vestibule of the buccal cavity of the patient and maintaining the dose in contact with the oral mucosa for a period of time sufficient for transmucosal absorption of a sufficient amount of estrogen to produce a therapeutically effective plasma concentration of estrogen. 00 LO CO 00 CM Q. Ill Bundesdruckerei Berlin 0 286 581 Description BUCCAL ADMINISTRATION OF ESTROGENS BACKGROUND OF THE INVENTION 5 Field of the invention: This invention relates to methods for administering drugs to human patients and more particularly to methods of administering estrogens. -
Evaluation of Mucoadhesion Properties of Different Polymers and Mucosal Tissues by Texture Analyser - Fatmanur Tugcu-Demiroz- Gazi University
Extended Abstract American Journal of Drug Delivery and Therapeutics 2020 Vol.7 No.13 Separation Techniques 2020: Evaluation of mucoadhesion properties of different polymers and mucosal tissues by texture analyser - Fatmanur Tugcu-Demiroz- Gazi University Fatmanur Tugcu-Demiroz Gazi University, Turkey Abstract Mucoadhesion is the capacity of materials to stick to mucosal Mucoadhesive polymers are a gathering of materials utilized in layers in the human body and give a transitory maintenance. various pharmaceutical frameworks. They are characterized as This property has been broadly used to create polymeric dose hydrophilic macromolecules, which contain various practical structures for buccal, oral, nasal, visual and vaginal medication natural gatherings ready to build up associations with mucosal conveyance. Incredible mucoadhesive properties are run of films. These polymers can be characterized by their the mill for hydrophilic polymers having charged gatherings communications with the mucosa. Non-covalent bonds and additionally non‐ionic utilitarian gatherings fit for shaping accepted to improve mucoadhesion incorporate hydrogen- hydrogen bonds with mucosal surfaces. This component article holding, hydrophobic cooperations, and electrostatic thinks about late advances in the investigation of connections. Mucoadhesive polymers might be cationic, mucoadhesion and mucoadhesive polymers. It gives a diagram anionic, or non-ionic. Anionic polymers, for example, on the structure of mucosal films, properties of bodily fluid poly(acrylic corrosive) derivates, are accepted to frame gels and the idea of mucoadhesion. Essential destinations hydrogen bonds beneath their pKa between their carboxylic behind the utilization of mucoadhesive medication conveyance gatherings and the hydroxyl gatherings of the bodily fluid gadgets are to delay their private time at the specific site to glycoprotein. -
Mucoadhesive and Rheological Studies on the Co-Hydrogel Systems of Poly(Ethylene Glycol) Copolymers with Fluoroalkyl and Poly(Acrylic Acid)
polymers Article Mucoadhesive and Rheological Studies on the Co-Hydrogel Systems of Poly(Ethylene Glycol) Copolymers with Fluoroalkyl and Poly(Acrylic Acid) Yang Sun, Adiel F. Perez , Ivy L. Cardoza , Nina Baluyot-Reyes and Yong Ba * Department of Chemistry and Biochemistry, California State University, Los Angeles, CA 90032, USA; [email protected] (Y.S.); [email protected] (A.F.P.); [email protected] (I.L.C.); [email protected] (N.B.-R.) * Correspondence: [email protected]; Tel.: +1-323-343-2360 Abstract: A self-assembled co-hydrogel system with sol-gel two-phase coexistence and mucoad- hesive properties was developed based on the combined properties of fluoroalkyl double-ended poly(ethylene glycol) (Rf-PEG-Rf) and poly(acrylic acid) (PAA), respectively. We have synthesized an Rf-PEG-g-PAA (where g denotes grafted) copolymer and integrated it into the Rf-PEG-Rf phys- ically cross-linked micellar network to form a co-hydrogel system. Tensile strengths between the co-hydrogel surfaces and two different sets of mucosal surfaces were acquired. One mucosal surface was made of porcine stomach mucin Type II, while the other one is a pig small intestine. The experi- mental results show that the largest maximum detachment stresses (MDSs) were obtained when the Rf-PEG-g-PAA’s weight percent in the dehydrated polymer mixture is ~15%. Tensile experiments also found that MDSs are greater in acidic conditions (pH = 4–5) (123.3 g/cm2 for the artificial mucus, Citation: Sun, Y.; Perez, A.F.; and 43.0 g/cm2 for pig small intestine) and basic conditions (pH = 10.6) (126.9 g/cm2, and 44.6 g.cm2, Cardoza, I.L.; Baluyot-Reyes, N.; Ba, respectively) than in neutral pH (45.4 g/cm2, and 30.7 g.cm2, respectively). -
CURRENT STATUS of BUCCAL DRUG DELIVERY SYSTEM: a REVIEW Srivastava Namita *, Monga Munish Garg R
Srivastava et al Journal of Drug Delivery & Therapeutics. 2015; 5(1):34-40 34 Available online on 15.01.2015 at http://jddtonline.info Journal of Drug Delivery and Therapeutics Open access to Pharmaceutical and Medical research © 2014, publisher and licensee JDDT, This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited REVIEW ARTICLE CURRENT STATUS OF BUCCAL DRUG DELIVERY SYSTEM: A REVIEW Srivastava Namita *, Monga Munish Garg R. V. Northland Institute, Chithera, Dadri, Gautama Buddha Nagar, Uttar Pradesh, India-203207 ABSTRACT Buccal mucosa is the preferred site for both systemic and local drug action. The mucosa has a rich blood supply and it relatively permeable. The buccal region of the oral cavity is an attractive target for administration of the drug of choice, particularly in overcoming deficiencies associated with the latter mode of administration. Problems such as first-pass metabolism and drug degradation in the gastrointestinal environment can be circumvented by administering the drug via the buccal route. Moreover, rapid onset of action can be achieved relative to the oral route and the formulation can be removed if therapy is required to be discontinued. It is also possible to administer drugs to patients who unconscious and less co-operative. In buccal drug delivery systems mucoadhesion is the key element so various mucoadhesive polymers have been utilized in different dosages form. Mucoadhesion may be defined as the process where polymers attach to biological substrate or a synthetic or natural macromolecule, to mucus or an epithelial surface. When the biological substrate is attached to a mucosal layer then this phenomenon is known as mucoadhesion. -
Buprenorphine / Naloxone Buccal Film
Buprenorphine/Naloxone Buccal Film Monograph Buprenorphine / Naloxone Buccal Film (BUNAVAIL) C-III National PBM Abbreviated Drug Review Sep 2014 VHA Pharmacy Benefits Management Services, Medical Advisory Panel, and VISN Pharmacist Executives The PBM prepares abbreviated reviews to compile information relevant to making formulary decisions. The manufacturer’s labeling should be consulted for detailed drug information. VA clinical experts may provide input on the content. Wider field review is not sought. Documents no longer current will be placed in the Archive section of www.pbm.va.gov. Executive Summary: Buprenorphine / naloxone buccal film (BUNAVAIL, by BioDelivery Sciences) was approved on 6 June 2014 by the Food and Drug Administration (FDA) for the maintenance treatment of opioid dependence, and should be used as part of a complete treatment plan to include counseling and psychosocial support. The main difference between buprenorphine / naloxone buccal film and sublingual tablets is a two-fold greater bioavailability due to greater absorption. Conclusions: Buprenorphine / naloxone buccal film produces buprenorphine bioavailabilities (systemic exposures) similar to those of SUBOXONE (buprenorphine / naloxone) sublingual tablets at approximately half the dose of buprenorphine. The more efficient absorption is achieved by using a trademarked BioErodible MucoAdhesive (BEMA®) technology. The manufacturer claims that the lower buprenorphine doses may “help to reduce the potential for misuse and diversion and potentially lessen the incidence of certain side effects” and that the buccal film may potentially overcome some of the challenges associated with sublingual administration. However, no clinical studies have been performed to support these claims. Potential clinical concerns with the buccal film include dosing and administration confusion when switching between the sublingual formulations and the buccal film, as well as look-alike, sound-alike name confusion with other buprenorphine-containing products. -
Mucoadhesiveness and Texture Profile Analysis of Doxycycline in Situ Hydrogels
ORIGINAL ARTICLES Faculty of Pharmaceutical Sciences1, Faculty of Odontology2, University of Iceland, Reykjavík, Iceland Evaluation of in vitro mucoadhesiveness and texture profile analysis of doxycycline in situ hydrogels V. G. R. PATLOLLA1,2, W. P. HOLBROOK2, S. GIZURARSON1, Þ. KRISTMUNDSDOTTIR1,* Received July 13, 2019, accepted September 23, 2019 *Corresponding Author: Þórdís Kristmundsdóttir, Faculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, 107 Reykjavik, Iceland [email protected] Pharmazie 75: 7-12 (2020) doi: 10.1691/ph.2020.9122 Delivery of active ingredients to the oral mucosa from topically applied formulations reduces side effects from systemic administration and enhances the treatment efficiency. The challenge however, is to maintain the formu- lation at the administration site due to rapid salivary flow and mechanical movements of the mouth. Therefore, addition of mucoadhesive polymers could aid in enhancing the formulation residence time by increasing the mucoadhesion capacity but this effect is negligible especially if low ratio of mucoadhesive polymers are added to the formulation. Different mucoadhesive polymers at 0.5% w/w (either single or combination of two polymers) were added to the hydrogels and tested for mucoadhesion capacity, tensile strengths, adhesiveness, cohe- siveness, compressibility and hardness. 0.5% povidone showed significantly highest work of mucoadhesion, 0.5% Carbopol formulation showed least cohesiveness and 0.5% HPMC showed highest adhesiveness, but a formulation containing a combination of 0.25% HPMC and 0.25% povidone showed the ideal parameters among all the mucoadhesive polymers tested. The effect of increase in concentration of HPMC (0.5, 1, 1.5, 2%) showed linear relationship for work of mucoadhesion and tensile strengths whereas for TPA the values were non-linear. -
Dr. Vijaya Khader Former Dean, Acharya N G Ranga Agricultural University Dr
Paper No. 1 : Novel Drug Delivery Systems I Module No 7 : Factors affecting mucoadhesion and evaluation techniques Development Team Prof. Farhan J Ahmad Principal Investigator Jamia Hamdard, New Delhi Dr. Vijaya Khader Former Dean, Acharya N G Ranga Agricultural University Dr. Zeenat Iqbal Paper Coordinator Jamia Hamdard, New Delhi Content Writer Dr. Zeenat Iqbal Jamia Hamdard, New Delhi ProfDr. KamlaA K Tiwarey Pathak ContentContent Reviewer PunjabiRajv academy University, of pharmacy, Patiala Mathura Prof. Dharmendra.C.Saxena Dr. Vijaya Khader SLIET, Longowal Dr. MC Varadaraj 1 Pharmaceutical Novel Drug Delivery Systems I sciences Factors affecting mucoadhesion and evaluation techniques Description of Module Subject Name Pharmaceutical Sciences Paper Name Novel Drug Delivery Systems I Module Name/Title Factors affecting mucoadhesion and evaluation techniques Module Id Pre-requisites Objectives Keywords Factors affecting mucoadhesion Polymer related factors 1) Hydrophilicity: Bioadhesive polymers having hydrophilic functional groups, such as carboxyl and hydroxyl interact with the mucosal surface via hydrogen bonding. On contact with the 2 Pharmaceutical Novel Drug Delivery Systems I sciences Factors affecting mucoadhesion and evaluation techniques aqueous media, the polymer swells, resulting in exposure of potential anchor sites. Further, the swollen polymers have got the maximum distance between their chains which leads to greater level of flexibility and penetration of the polymer in the mucosa. 2) Molecular weight: The mucoadhesive ability of the polymer depends on its molecular weight. The bioadhesive force of the polymer increases up to 100,000 with the molecular weight. However, no further enhancement is observed beyond this value. 3) Cross linking and swelling: the density of cross linking density of the polymer is inversely related to its swelling. -
Medication Administration
MEDICATION ADMINISTRATION GENERAL CONSIDERATIONS A. Before administering any medication, the EMT should know: 1. What is the medication being used? 2. Does the patient have an allergy to this medication? 3. What is the safe and effective dose? 4. What is the correct administration route? 5. What are the indications? (Why are you using is?) 6. What are the contraindications? (Why or when would you NOT use this medication?) 7. What are the expected effects? 8. What are the adverse effects / side effects? 9. Is the medication expired? B. The “Six Rights” of medication administration: 1. Right patient – is the medication indicated for this patient; no contraindications; no allergies 2. Right drug – the correct name (trade name vs. generic name); correct concentration 3. Right dose 4. Right route 5. Right time – slow IVP vs. rapid IVP 6. Right documentation C. Correct documentation of medications administered and/or IV/IO placement will include: 1. Time of medication administration; IV/IO placement 2. Route of administration 3. Size of catheter (IV/IO) 4. Site location for IV/IO and SQ, IM medication (include unsuccessful IV/IO attempt locations) 5. Dose or volume infused 6. Time of infusion as indicated (e.g., rapid IVP, infused over 10 minutes, etc.) 7. Name of EMT responsible 8. Any complications and steps made to correct 9. Patient’s response to treatment D. Use of a medication simply because it is in the protocol is not an acceptable standard of medical care. When there are questions about medication administration, consult medical control. ORAL ADMINSTRATION To administer an oral (PO) medication ensure that the patient has an intact gag reflex and place the patient in a seated or semi-seated position.