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.

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 FORMULATION AND EVALUATION OF FAST DISSOLVING TABLET OF APREPITANT BY USING NATURAL AND SYNTHETIC SUPERDISINTEGRANTS

2019 ◽  
pp. 64-71
Author(s):  
RAJNI BALA ◽  
SHAILESH SHARMA ◽  
IKGPTU
Keyword(s):  
Compression Method ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Sodium Starch Glycolate ◽  
First Pass Metabolism ◽  
First Pass ◽  
Croscarmellose Sodium ◽  
Improve Patient ◽  
Pass Metabolism ◽  
Natural And Synthetic

Objective: The present study was aimed to formulate fast dissolving tablets (FDTs) of Aprepitant (APT) using natural and synthetic superdisintegrants with the desired onset of action, increased bioavailability by reducing the frequency of dosage and also reduce the first-pass metabolism of the drug. Methods: In this research, the gum isolated from cordia dichotoma was investigated as super disintegrants in fast dissolving tablets (FDTs). The aprepitant tablets were prepared separately using cordia dichotoma (natural), sodium starch glycolate and croscarmellose sodium (synthetic) as superdisintegrants by direct compression method. The tablets were evaluated for various precompression and post-compression parameters. Results: The optimized formulation (APT F3) of cordia dichotoma (8%) showed satisfactory physicochemical properties, minimum disintegration time (34 seconds) and highest dissolution rate (86.52%) in 10 min than the other synthetic superdisintegrants. Also, the pharmacokinetic study of the optimized formulation showed effective results as compared with marketed product of aprepitant. Conclusion: The developed formulation can improve the onset of action as well as improve patient compliance.

scholarly journals Curcumin Innovative Delivery Forms: Paving the ‘Yellow Brick Road’ of Antitumoral Phytotherapy

2020 ◽  
Vol 10 (24) ◽  
pp. 8990
Author(s):  
Magda Carvalho Henriques ◽  
Maria Amparo F. Faustino ◽  
Susana Santos Braga
Keyword(s):  
Biological Activity ◽  
Historical Perspective ◽  
Chemical Properties ◽  
Routes Of Administration ◽  
Raising Awareness ◽  
Physico Chemical ◽  
First Pass Metabolism ◽  
First Pass ◽  
Antitumor Properties ◽  
Pass Metabolism

This review deals with the various aspects involved in the medicinal action of curcumin, from the photosensitivity and its relevance to storage and shelf-life, to the different routes of administration, which influence the bioavailability. The focus of the review is on the antitumor properties of curcumin and the currently available solutions for their amelioration. The work starts by presenting a brief historical perspective on the origins and uses of curcumin, from early days until the present time. The following sections describe the physico-chemical properties of curcumin and their impact on the biological activity and pharmacokinetics, raising awareness to the need for formulations able to improve the bioavailability. The last section is focused on research efforts being made to circumvent curcumin’s instability and low availability due to the extensive hepatic first pass metabolism, describing innovative scientific advances and new patented formulations and emerging products on the market.

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.

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.

scholarly journals Formulation And Evaluation of Fast Dissolving Oral Films Incorporated With Ramipril and β-Cyclodextrin Complex

2020 ◽  
pp. 390-395
Author(s):  
Puttaswamy Nirmala
Keyword(s):  
Cyclodextrin Complex ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Drug Content ◽  
Bcs Class Ii ◽  
First Pass Metabolism ◽  
First Pass ◽  
Oral Films ◽  
Low Solubility ◽  
Pass Metabolism

Ramipril being ACE inhibitor belongs to BCS class II drug with low solubility and undergoes first-pass metabolism that leads to reduced bioavailability of 28%. The current research is aimed at formulating and evaluating ramipril fast dissolving oral films (FDOF). Solubility enhancement of ramipril was done by formation of   inclusion complex with β-cyclodextrin in 3 ratios (1:0.5, 1:1, 1:2). Based on higher drug content and dissolution values the physical mixture of ramipril with β-cyclodextrin in 1:1 ratio (IC2) was chosen for further studies. Total 12 formulations of ramipril FDOF containing IC2 prepared with various polymers and evaluated for physicochemical properties. The optimized formulation F9 shown better tensile strength (11.6 g/cm2), significant % elongation (9.8) and maximum % drug content of 99.98 %. The formulation F9 exhibited minimum disintegration time of 9 sec that is desirable for immediate onset of action and maximum drug release. The FTIR data of F9 assured the compatibility of drug and formulation excipients, found to be stable for 180 days at accelerated conditions. The study confirmed that ramipril FDOF lead to quicker onset of action and enhanced therapeutic efficiency in comparison to marketed product.

scholarly journals Formulation and evaluation of fast dissolving tablet of albendazole

2012 ◽  
Vol 1 (10) ◽  
pp. 311-316 ◽  
Author(s):  
Devendra Revanand Rane ◽  
Hemant Narhar Gulve ◽  
Vikas Vasant Patil ◽  
Vinod Madhaorao Thakare ◽  
Vijay Raghunath Patil
Keyword(s):  
Dissolution Rate ◽  
Microcrystalline Cellulose ◽  
Broad Spectrum ◽  
Pharmaceutical Journal ◽  
Direct Compression ◽  
Onset Of Action ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Albendazole is broad spectrum anthelmintic use against many helminths. It is used for treatment of Threadworm, Hookworm, and Tapeworm. It has low bioavailability due to its first pass metabolism.  In the present work, fast dissolving tablet of Albendazole was design with a view to and provide a quick onset of action. The main objective of the study was to formulate fast dissolving tablets of Albendazole to achieve a better dissolution rate and further improving the bioavailability of the drug. Fast dissolving tablets prepared by direct compression and using super disintegrants in different concentration and evaluated for the pre-compression parameters. The prepared tablets were evaluated for post compressional evaluation. Among all, the formulation F3 containing 5%w/w superdisintegrant Crospovidone and 20%w/w Microcrystalline Cellulose was considered to be best formulation, which release up to 99.097% in 40 min.DOI: http://dx.doi.org/10.3329/icpj.v1i10.11848 International Current Pharmaceutical Journal 2012, 1(10): 311-316 

scholarly journals Parenteral systems for statin delivery: a review

2019 ◽  
Vol 18 (1) ◽  
Author(s):  
Shahla Korani ◽  
Samira Bahrami ◽  
Mitra Korani ◽  
Maciej Banach ◽  
Thomas P. Johnston ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Oral Route ◽  
Delivery Methods ◽  
Routes Of Administration ◽  
First Pass Metabolism ◽  
First Pass ◽  
Convenient Route ◽  
Statin Drugs ◽  
Alternative Delivery ◽  
Pass Metabolism

Abstract The oral route of drug administration is the most common and convenient route for dosing statin drugs, and, in fact, most medications, because of ease of drug delivery, patient compliance, and cost-effectiveness. However, the oral administration of statin drugs has disadvantages such as hepatic first-pass metabolism and degradation within the gastrointestinal tract that limit their overall bioavailability. This review introduces several diverse non-oral delivery methods for the administration of statins. These alternative delivery systems and routes of administration are varied and are capable of improving the bioavailability and therapeutic efficacy of statin drugs.

scholarly journals Formulation and Characterization of Isradipine Nanoparticle for Dissolution Enhancement

2021 ◽  
Vol 30 (1) ◽  
pp. 218-225
Author(s):  
Rawaa M. Hussien ◽  
Mowafaq M. Ghareeb
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Poloxamer 407 ◽  
In Vitro Dissolution ◽  
Dissolution Enhancement ◽  
Drug Bioavailability ◽  
Particle Size Reduction ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Isradipine belong to dihydropyridine (DHP) class of calcium channel blockers (CCBs). It is  used in the treatment of hypertension, angina pectoris, in addition to Parkinson disease. It goes under the BCS class II drug (low solubility-high permeability). The drug will experience extensive first-pass metabolism in liver, therefore, oral bio-availability will be approximately15 to 24 %.    The aim of this study was to formulate and optimize a stable  nanoparticles of a highly hydrophobic drug, isradipine by anti-solvent microprecipitation Method to achieve the higher in vitro dissolution rate, so that it will be absorbed by intestinal lymphatic transport in order to avoid hepatic first-pass metabolism  and improve drug bioavailability.   Twenty one formulas of Isradipine nanoparticles were prepared by antisolvent precipitation method utilizing one of these polymers (Poloxamer 188, PVP-k30, HPMC E5, PVA, Poloxamer 407, and Soluplus) at different drugs: polymer ratios. The polymer type, the drug to polymer ratio, ultrasonication power and the effect of addition of co-stabilizer on the particle size, and polydispersity index (PDI)  were investigated.   Among all the prepared nanoparticles formulas, formula (F9) which contain Soluplus as a stabilizer at polymer: drug ratio of (1:0.75) and solvent: antisolvent ratio of (1:9) was considered as the optimum formula which shows good evaluation parameters in addition to the increment in the solubility to about 10 times than that of the pure drug. The investigations of the drug–excipients compatibility studies by FTIR and DSC, crystalline state by P-XRD, surface morphology by SEM were done. Moreover, the analysis by DSC and SEM of the nanoparticles of the selected formula (F12) indicate a reduction in the crystallinity and amorphization of the drug. It can be concluded that the dissolution rate of Isradipine was significantly increased through particle size reduction to nanosize.            

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