Microemulsions for Nasal Drug Delivery Systems: An Overview

2013 ◽  
Vol 5 (4) ◽  
pp. 1825-1831
Author(s):  
Hitendra S. Mahajan ◽  
Rasal A D
Keyword(s):  
Nasal Delivery ◽  
Microemulsion System ◽  
Nasal Drug Delivery ◽  
Nasal Route ◽  
Solubilization Capacity ◽  
First Pass Metabolism ◽  
First Pass ◽  
The Brain ◽  
Pass Metabolism ◽  
Selection Of

Most drugs cannot be given orally because of significant degradation in the GIT or first pass metabolism in the liver. Nasal route for the delivery of some drugs offers an alternative in the pharmaceutical industry. The present review deals with the utility of the nasal route for the delivery of drugs to the brain as a microemulsion system in the treatment of a number of ailments like migraine, epilepsy, and hypertension. The nasal route could be important for drugs that are used in crisis treatments, such as for pain, and for centrally acting drugs where the pathway from nose to brain might provide a faster and more specific therapeutic effect. The purpose of the article is to provide an overview of the concept of microemulsion, selection of surfactant, co-surfactant, oils, formulation of microemulsion, phase diagram study, and evaluation of microemulsion. The review also focuses on the excipients available for formulation of microemulsions for nasal delivery and describes the investigations reported for the various classes of therapeutic agents. The interesting features of microemulsion such as spontaneity of formation, ease of manufacturing, high solubilization capacity and self-preserving properties make them the vehicle of choice for nasal delivery.

Computer simulations for bioequivalence trials: Selection of analyte in BCS drugs with first-pass metabolism and two metabolic pathways

2010 ◽  
Vol 41 (5) ◽  
pp. 716-728 ◽  
Author(s):  
Carmen Navarro-Fontestad ◽  
Isabel Gonzalez-Alvarez ◽  
Carlos Fernández-Teruel ◽  
Alfredo Garcia-Arieta ◽  
Marival Bermejo ◽  
...  
Keyword(s):  
Computer Simulations ◽  
Metabolic Pathways ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism ◽  
Selection Of

scholarly journals Optimization of ThermoreversibleIn SituNasal Gel of Timolol Maleate

Scientifica ◽  
2016 ◽  
Vol 2016 ◽  
pp. 1-11 ◽  
Author(s):  
Swati Jagdale ◽  
Nirupama Shewale ◽  
Bhanudas S. Kuchekar
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Ex Vivo ◽  
Nasal Delivery ◽  
Poloxamer 407 ◽  
Timolol Maleate ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Nasal route had shown better systemic bioavailability due to its large surface area, porous endothelial membrane, high total blood flow, and avoidance of first-pass metabolism. Timolol maleate is a beta blocker used primarily in the treatment of hypertension. Drug undergoes extensive hepatic first-pass metabolism (80%). The drug has half-life of 4 hrs. Oral bioavailability of timolol maleate is 61%. The aim of the present study was to optimize controlled releasein situnasal delivery for timolol maleate. HPMC and Poloxamer 407 were selected as polymer in formulation of thermoreversiblein situnasal gel. Optimization was carried out using 32factorial design. It was observed that formulations f1 and f4 revealed the highest % drug release, that is, 93.57% and 91.66%, respectively. Factorial design study indicated that the drug release and viscosity were most significant dependent factors.Ex vivodiffusion study through nasal mucosa indicated 67.26 ± 2.10% and 61.07 ± 2.49% drug release for f1 and f4 formulations. f1 was the optimized batch. This batch thus can act as a potential nasal delivery with enhanced bioavailability for the drug.

Drugs and other physical treatments

Psychiatry ◽  
2019 ◽  
Author(s):  
Rebecca McKnight ◽  
Jonathan Price ◽  
John Geddes
Keyword(s):  
Psychotropic Drugs ◽  
Psychological Treatment ◽  
Plasma Concentrations ◽  
Parent Drug ◽  
Portal System ◽  
First Pass Metabolism ◽  
First Pass ◽  
Physical Treatments ◽  
The Brain ◽  
Pass Metabolism

This chapter is about the use of drugs and electroconvul­sive therapy (ECT). Stimulants for ADHD are covered in Chapter 32, and psychological treatments in Chapter 14. This is a convenient way of dividing the subject matter of a book, but in practice these physical treatments should always be combined with psychological treatment, unless the patient chooses not to undertake this. The account in this chapter is concerned with prac­tical therapeutics rather than basic pharmacology, and it will be assumed that the reader has studied the basic pharmacology of the principal types of drug used in psychiatric disorders (readers who do not have this knowledge should consult a textbook, see, for example, ‘Further reading’). Nevertheless, a few important points about the actions of psychotropic drugs will be con­sidered, before describing the specific groups of drugs (see Science box 13.1). To be effective, psychotropic drugs must reach the brain in adequate amounts. How far they do this depends on their absorption, metabolism, excretion, and passage across the blood– brain barrier. Most psychotropic drugs are absorbed readily from the gut, but absorption can be reduced by intestinal hurry or a malabsorption syndrome. Absorption can be slowed down by use of enteric coatings on capsules, should the clinician wish for a drug to be delivered over a longer period of time. Most psychotropic drugs are metabolized partially in the liver on their way from the intestine via the portal system to the systemic circulation. The amount of this so- called first- pass metabolism differs from one person to another, and it is altered by certain drugs, taken at the same time, which induce liver enzymes (e.g. carbamazepine) or inhibit them (e.g. MAOIs). Although first- pass metabolism reduces the amount of the original drug reaching the brain, the metabolites of some drugs have their own therapeutic effects. As many psychotropic drugs have active metabolites, the measurement of plasma concentrations of the parent drug is generally a poor guide to treatment.

scholarly journals CRITICAL ANALYSIS OF PURVA KARMA PRIOR TO NASYA W.S.R. SNEHA NASYA

2020 ◽  
pp. 94-97
Author(s):  
Divya Virupaksha ◽  
Krishnan N ◽  
Ajoy Viswam ◽  
Naveen B. S
Keyword(s):  
The Body ◽  
Nasal Delivery ◽  
Drug Preparation ◽  
Drug Degradation ◽  
First Pass Metabolism ◽  
First Pass ◽  
Gastro Intestinal Tract ◽  
Slow Absorption ◽  
Pass Metabolism

Ayurveda Panchakarmas are an all-time big name for both Ayurveda doctors and patients. Their efficacy of targeting the body holistically and evacuating toxins, thereby, addressing most of the problems of an individual makes it a hit. This paper aims at estimating the contribution of Purva Karma (procedures prior to instillation of medicine) in the outcome, especially in the context of Sneha Nasya (instillation of unctuous medicine). Nasal route of administration may help address the hitches accompanying to poor bioavailability, slow absorption, drug degradation, and possible adverse events in the gastro intestinal tract and avoids the first-pass metabolism in the liver. However, when considering nasal delivery, appropriate measures need to be taken to address the limitations of drug delivery in this region. Purva Karma starts with drug preparation and ends with stage of instillation of medicine (8 check points). The role of each of them on overcoming the limitations and delivering the results is reviewed.

scholarly journals Critical Review of Lipid-Based Nanoparticles as Carriers of Neuroprotective Drugs and Extracts

Nanomaterials ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 563
Author(s):  
Filipe Fernandes ◽  
Mónica Dias-Teixeira ◽  
Cristina Delerue-Matos ◽  
Clara Grosso
Keyword(s):  
Brain Parenchyma ◽  
Drug Bioavailability ◽  
Onset Of Action ◽  
Routes Of Administration ◽  
Neuroprotective Drugs ◽  
First Pass Metabolism ◽  
First Pass ◽  
The Central Nervous System ◽  
The Brain ◽  
Pass Metabolism

The biggest obstacle to the treatment of diseases that affect the central nervous system (CNS) is the passage of drugs across the blood-brain barrier (BBB), a physical barrier that regulates the entry of substances into the brain and ensures the homeostasis of the CNS. This review summarizes current research on lipid-based nanoparticles for the nanoencapsulation of neuroprotective compounds. A survey of studies on nanoemulsions (NEs), nanoliposomes/nanophytosomes and solid lipid nanoparticles (SLNs)/nanostructured lipid carriers (NLCs) was carried out and is discussed herein, with particular emphasis upon their unique characteristics, the most important parameters influencing the formulation of each one, and examples of neuroprotective compounds/extracts nanoencapsulated using these nanoparticles. Gastrointestinal absorption is also discussed, as it may pose some obstacles for the absorption of free and nanoencapsulated neuroprotective compounds into the bloodstream, consequently hampering drug concentration in the brain. The transport mechanisms through which compounds or nanoparticles may cross BBB into the brain parenchyma, and the potential to increase drug bioavailability, are also discussed. Additionally, factors contributing to BBB disruption and neurodegeneration are described. Finally, the advantages of, and obstacles to, conventional and unconventional routes of administration to deliver nanoencapsulated neuroprotective drugs to the brain are also discussed, taking into account the avoidance of first-pass metabolism, onset of action, ability to bypass the BBB and concentration of the drug in the brain.

scholarly journals PREVENTIVE AND CURATIVE ASPECT OF DHUMNASYA (NASAL INSUFFLATION OF MEDICATED SMOKE)

2021 ◽  
Vol p5 (6) ◽  
pp. 3135-3142
Author(s):  
Tanuja Mehta ◽  
Uttam Kumar Sharma ◽  
Bhawana Mittal ◽  
Shikha Pandey
Keyword(s):  
Drug Degradation ◽  
Effective Manner ◽  
Systemic Level ◽  
Different Types ◽  
First Pass Metabolism ◽  
First Pass ◽  
The Brain ◽  
Slow Absorption ◽  
Pass Metabolism

Background- Panchkarma is a group of procedures known for its preventive, promotive, prophylactic and rejuve- nating properties as well as radicle cure. Nasya is one of the Panchkarma treatments. Among the various forms of Nasya, Dhumnasya is a very effective type of Nasya which has further been classified into different types based on various potency of herbs with their respective properties. Aim and Objective: To find out the role of Dhumnasya in the preventive and curative aspects. Material and Methods: Classics of Ayurveda having references regarding Nasya, Modern literature, published articles in peer-reviewed journals, published books and subject-related material available online have been screened, compiled, organized and described systematically. Result: In Dhumnasya medicinal herbs with other constituents are burnt in such an effective manner to produce a medicated fume contain- ing volatile phytochemical of herbs, which when inhaled through nasal route exerts their efficient role in both pre- vention and treatment of various forms of disease both at a local and systemic level. Conclusion: In this review article, it has been tried to focus on the preventive and curative aspect of Dhumnasya so to help to address issues related to poor bioavailability, slow absorption, drug degradation and adverse event in the GIT tract and avoid the first-pass metabolism in the liver and discover the advantage of smoke based therapies as rapid delivery to the brain, more efficient pulmonary absorption and become the suitable substitute for the oral and parental administration. Keywords: Panchkarma, Dhumnasya, Nasya, Medicated smoke.

Ligand Conjugated Targeted Nanotherapeutics for Treatment of Neurological Disorders

2020 ◽  
Vol 26 (19) ◽  
pp. 2291-2305 ◽  
Author(s):  
Saurabh Mittal ◽  
Muhammad U. Ashhar ◽  
Farheen F. Qizilbash ◽  
Zufika Qamar ◽  
Jasjeet K. Narang ◽  
...  
Keyword(s):  
Neurological Disorders ◽  
Neurological Diseases ◽  
Therapeutic Agents ◽  
Review Article ◽  
Brain Delivery ◽  
Intranasal Route ◽  
First Pass Metabolism ◽  
First Pass ◽  
The Brain ◽  
Pass Metabolism

Background: Human brain is amongst the most complex organs in human body, and delivery of therapeutic agents across the brain is a tedious task. Existence of blood brain barrier (BBB) protects the brain from invasion of undesirable substances; therefore it hinders the transport of various drugs used for the treatment of different neurological diseases including glioma, Parkinson's disease, Alzheimer's disease, etc. To surmount this barrier, various approaches have been used such as the use of carrier mediated drug delivery; use of intranasal route, to avoid first pass metabolism; and use of ligands (lactoferrin, apolipoprotein) to transport the drug across the BBB. Ligands bind with proteins present on the cell and facilitate the transport of drug across the cell membrane via. receptor mediated, transporter mediated or adsorptive mediated transcytosis. Objective: The main focus of this review article is to illustrate various studies performed using ligands for delivering drug across BBB; it also describes the procedure used by various researchers for conjugating the ligands to the formulation to achieve targeted action. Methods: Research articles that focused on the used of ligand conjugation for brain delivery and compared the outcome with unconjugated formulation were collected from various search engines like PubMed, Science Direct and Google Scholar, using keywords like ligands, neurological disorders, conjugation, etc. Results and Conclusion: Ligands have shown great potential in delivering drug across BBB for treatment of various diseases, yet extensive research is required so that the ligands can be used clinically for treating neurological diseases.

Identification of a Cranberry Juice Product Capable of Inhibiting Enteric CYP3A-Mediated First-Pass Metabolism in Humans

Planta Medica ◽  
2008 ◽  
Vol 74 (03) ◽  
Author(s):  
N Ngo ◽  
Z Yan ◽  
TN Graf ◽  
DR Carrizosa ◽  
EC Dees ◽  
...  
Keyword(s):  
Cranberry Juice ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Development, Characterization and Optimization of Mucoadhesive Tablet for Buccal Delivery of Domperidone

2019 ◽  
Vol 9 (1) ◽  
pp. 37-49
Author(s):  
Jagdale Sachin ◽  
Panbude Aishwarya ◽  
Navasare Priya
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Research Work ◽  
Wet Granulation ◽  
Buccal Delivery ◽  
Scanning Calorimetry ◽  
Mucoadhesive Polymers ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Background and Objective: Upon oral administration domeperidone is rapidly absorbed, but subjected to the first pass effect which lowers systemic bioavailability to 15%. Mucoadhesive tablet can remain attached to buccal mucosa and becomes capable of bypassing hepatic first-pass metabolism to improve absorption directly into systemic circulation. The present research work was carried with an aim to develop, evaluate and optimize mucoadhesive tablet containing domperidone (DOME) for buccal delivery using different bio-adhesive polymeric combinations. </P><P> Methods: The buccal tablets were formulated by wet granulation method using isopropyl alcohol. The preliminary formulations were prepared using combinations of HPMC K4, HPMC K15, HPMC K100, HPMC E5 as mucoadhesive polymers. 32 full factorial design was applied to determine the effect of independent variables like concentration of mucoadhesive polymers (HPMC K15 and HPMC K100) over dependent variables like mucoadhesive properties (swelling index, bioadhesive strength and in vitro drug release). The prepared mucoadhesive tablets were evaluated for their tablet properties and mucoadhesive properties. The interactions between drug and polymers were studied by Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC). </P><P> Results: All formulations of factorial design showed satisfactory physicochemical, mechanical and bioadhesive characteristics. The formulation F9 exhibited maximum cumulative drug release, mucoadhesive strength and swelling index. Conclusion: The developed buccal tablet of domperidone might prove alternative to bypass the hepatic first pass metabolism and to avoid degradation which in turn may result in reducing the frequency of administration. Thus, mucoadhesive tablet of domeperidone may become viable alternative overcoming the side effects; achieving greater therapeutic effectiveness and improving the patient compliance.

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