Parenteral systems for statin delivery: a review

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.

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Solid lipid nanocarriers as alternative drug delivery system for improved oral delivery of drugs

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v10i6-s.4410 ◽

2020 ◽

Vol 10 (6-s) ◽

pp. 168-172

Author(s):

Gorre Thirupathi ◽

Samanthula Kumara Swamy ◽

Alli Ramesh

Keyword(s):

Oral Bioavailability ◽

Oral Delivery ◽

Lipid Nanoparticles ◽

Delivery Systems ◽

Chemical Degradation ◽

Solid Lipid ◽

First Pass Metabolism ◽

First Pass ◽

Lipid Nanocarriers ◽

Pass Metabolism

Oral bioavailability of drugs is mainly limited due to the poor aqueous solubility, enhanced chemical degradation, reduced permeation and/or first pass metabolism. Various novel delivery systems are developed for improved oral bioavailability of these drugs such as modified orals, buccal, transdermal and osmotic delivery systems. Colloidal carrier systems such as nanoparticles, lipid nanoparticles, nanoemulsions, microspheres, liposomes, resealed erythrocytes and transfersomes were also developed to enhance the oral delivery. Among these, solid lipid nanocarriers (SLNs) also gain much attention on the enhancement of oral bioavailability. SLNs are submicron sized nanoparticles and composed of solid lipid, surfactants and cosurfactants. The enhanced oral bioavailability of poorly soluble drugs from SLNs might be due to the reduced particle size, bypassed presystemic metabolism, and enhanced gastric mucosa permeability. Vast literature is available for the advantages, limitations, preparation methods, evaluation parameters and application of SLNs in different routes. This review mainly focused on list of drugs developed as SLNs and considered as an alternative approach to enhance the oral bioavailability based on pharmacokinetic as well as pharmacodyanmic parameters was discussed. Keywords: Oral bioavailability, solubility, first-pass metabolism, solid lipid nanoparticles, pharmacokinetics, pharmacodynamics.

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Potential Nanospray Inhalation of Remdesivir and Hydroxychloroquine using Poly (lactic-co-glycolic) Acid as Fast Delivery for Covid-19 Treatment.

Journal of Pharmacy ◽

10.31436/jop.v1i1.50 ◽

2021 ◽

Vol 1 (1) ◽

pp. 34-44

Author(s):

Muhammad Taher ◽

Siti Syazwani Shaari ◽

Deny Susanti

Keyword(s):

Drug Delivery ◽

Glycolic Acid ◽

Review Article ◽

Converting Enzyme ◽

Dry Powder Inhalation ◽

First Pass Metabolism ◽

First Pass ◽

Site Of Action ◽

Alternative Delivery ◽

Pass Metabolism

Introduction: The oral medication of remdesivir and hydroxychloroquine face several limitations in covid-19 therapy. Despite having the first-pass metabolism, it also has a limitation in the patient who has hospitalised with a severe covid-19 infection. It is especially for a drug that is targeting the angiotensin-converting enzyme II (ACE2) receptor where the receptors are found abundantly in the lung, kidney, heart, and gastrointestinal tract. Therefore, an alternative delivery such as nanospray inhalation would provide a great benefit to those patients. Methods: Scientific sources from Scopus, PubMed, Google Scholar, EBSCO, ScienceDirect, and Elsevier were accessed for publication of this review article regarding the nanospray inhalation for Covid-19. Results: Since the main organ infected by SARS-CoV-2 is the esophagus and lung, inhalation may be the best route to deliver the drug to the site of action. It is proposed that poly (lactic-co-glycolic) acid to be used in the formulation. Conclusion: Poly (lactic-co-glycolic) acid (PLGA) is considered a suitable polymer since it is biocompatible and noncytotoxic, it is the most widely applied in drug delivery either as carrier or excipient for the optimal formulation and distribution of the drugs. Dry powder inhalation of remdesivir and hydroxychloroquine may be an alternative way to deliver the drug against Covid-19.

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High-Payload Buccal Delivery System of Amorphous Curcumin–Chitosan Nanoparticle Complex in Hydroxypropyl Methylcellulose and Starch Films

International Journal of Molecular Sciences ◽

10.3390/ijms22179399 ◽

2021 ◽

Vol 22 (17) ◽

pp. 9399

Author(s):

Li Ming Lim ◽

Kunn Hadinoto

Keyword(s):

Oral Delivery ◽

Hydroxypropyl Methylcellulose ◽

Buccal Delivery ◽

Limited Effectiveness ◽

First Pass Metabolism ◽

First Pass ◽

Starch Films ◽

Hydroxypropyl Starch ◽

High Payload ◽

Pass Metabolism

Oral delivery of curcumin (CUR) has limited effectiveness due to CUR’s poor systemic bioavailability caused by its first-pass metabolism and low solubility. Buccal delivery of CUR nanoparticles can address the poor bioavailability issue by virtue of avoidance of first-pass metabolism and solubility enhancement afforded by CUR nanoparticles. Buccal film delivery of drug nanoparticles, nevertheless, has been limited to low drug payload. Herein, we evaluated the feasibilities of three mucoadhesive polysaccharides, i.e., hydroxypropyl methylcellulose (HPMC), starch, and hydroxypropyl starch as buccal films of amorphous CUR–chitosan nanoplex at high CUR payload. Both HPMC and starch films could accommodate high CUR payload without adverse effects on the films’ characteristics. Starch films exhibited far superior CUR release profiles at high CUR payload as the faster disintegration time of starch films lowered the precipitation propensity of the highly supersaturated CUR concentration generated by the nanoplex. Compared to unmodified starch, hydroxypropyl starch films exhibited superior CUR release, with sustained release of nearly 100% of the CUR payload in 4 h. Hydroxypropyl starch films also exhibited good payload uniformity, minimal weight/thickness variations, high folding endurance, and good long-term storage stability. The present results established hydroxypropyl starch as the suitable mucoadhesive polysaccharide for high-payload buccal film applications.

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

Applied Sciences ◽

10.3390/app10248990 ◽

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.

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Core-in-cup/liquisol dual tackling effect on azelnidipine buccoadhesive tablet micromeritics, in vitro release, and mucoadhesive strength

Acta Pharmaceutica ◽

10.2478/acph-2019-0022 ◽

2019 ◽

Vol 69 (3) ◽

pp. 381-398

Author(s):

Amira A. Rashad ◽

Sara Nageeb El-Helaly ◽

Randa T. Abd El Rehim ◽

Omaima N. El-Gazayerly

Keyword(s):

In Vitro Release ◽

Aqueous Solubility ◽

Oral Route ◽

Wet Granulation ◽

Preparation Technique ◽

First Pass Metabolism ◽

First Pass ◽

Vitro Release ◽

Pass Metabolism

Abstract Reduced bioavailability of azelnidipine is related to its poor aqueous solubility and extensive first-pass metabolism, which hinder its efficacy. These problems were addressed by implementing (1) a liquisol technique for promoting the dissolution rate in a controlled-release manner and (2) a core-in-cup bucco-adhesive drug delivery system as an alternative to the oral route. A 33 factorial design was used to study the effects of polymer type (sodium carboxymethyl cellulose (CMC Na), chitosan, or Carbomer P940) concentration (5, 10 or 15 %) and preparation technique (simple mix, liquisol or wet granulation) on the dissolution and mucoadhesion of core-in-cup azelnidipine buccoadhesive tablets. Tablet micromeritics, swelling index, mucoadhesive strength and in vitro release were characterized. Statistical analyses of these factors show ed significant effects on the studied responses, where F#16 prepared by the liquisol technique and containing 15 % CMC Na was chosen with an overall desirability of 0.953.

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

Nanomaterials ◽

10.3390/nano11030563 ◽

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.

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A Glance on Mucoadhesive System - Still more to Understand

Research Journal of Science and Technology ◽

10.52711/2349-2988.2021.00020 ◽

2021 ◽

pp. 133-141

Author(s):

Pawan S. Avhad ◽

Revati Gupta ◽

Swati S. Rawat ◽

Raghvendra S. Dubey

Keyword(s):

Drug Delivery ◽

Oral Route ◽

Basic Knowledge ◽

Drug Penetration ◽

Mucoadhesive Polymers ◽

First Pass Metabolism ◽

First Pass ◽

Good Patient Compliance ◽

Pass Metabolism ◽

Proteins And Peptides

Most popular and useful route of administration is oral one, among that mucoadhesive system is also preferable. This system is interact with mucus layer containing epithelial cell and mucin molecules which improves the contact time of dosage form, leading to improvement in both local and systemic effects. There are various routes of mucoadhesive drug delivery system, oral route is the most oldest and preferred by patient being convenient to use. However peroral route has some disadvantages such as hepatic first pass metabolism and enzymatic degradation in GIT which is a hindrance to the absorption of most proteins and peptides groups of drugs. The mucosa of the oral cavity contains an intimidating barrier to drug penetration, and one method of optimizing drug delivery is by the use of adhesive dosage forms and the mucosa is connected with various blood supplies by which it is permeable. This route has quick action, and good patient compliance with pediatric and old age patients. The buccal cavity is very easier for a bioadhesion system because of a smooth and relatively immobile surface and accessibility. Mucoadhesion can be achieved by using various mucoadhesive polymers. There are various types of mucoadhesive polymers which improves bioadhesion. Also various theories are referred to clear the concept of mucoadhesion, such as diffusion, facture, electronic and adsorption theories. This article contains definition, mechanism, advantage, and disadvantage. In this article we are going to overlook basic knowledge about mucoadhesion and its formulations.

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Orodental Local Drug Delivery

Journal of Health Sciences & Research ◽

10.5005/jp-journals-10042-1019 ◽

2015 ◽

Vol 6 (2) ◽

pp. 41-46 ◽

Cited By ~ 1

Author(s):

Nandita Ahanthem ◽

Nikhat Gazge

Keyword(s):

Drug Delivery ◽

Drug Dosage ◽

Oral Route ◽

Local Drug Delivery ◽

Systemic Delivery ◽

Rapid Repair ◽

First Pass Metabolism ◽

First Pass ◽

Pass Metabolism ◽

Systemic Drug

ABSTRACT Oral mucosal diseases are the most common diseases affecting humans and these can be treated with the use of various drugs. These drugs can be administered via many routes to produce its pharmacological bioeffects. One such site is the oral cavity, where both local and systemic deliveries of drug can take place. Oral route has been the most convenient and commonly employed route of drug delivery. The oral mucosa's accessibility, excellent blood supply, bypass of hepatic first pass metabolism, rapid repair, and permeability profile make it an attractive site for local and systemic drug deliveries. Local drug delivery allows topical treatment of various oral mucosal diseases, as it provides a more targeted and efficient drug-delivery option than systemic delivery. This review highlights various methods of drug delivery and important aspects of mucoadhesive drug delivery and drug dosage for treatment of orodental diseases. How to cite this article Ahanthem N, Basavaraju SM, Pachipulusu B, Gazge N. Orodental Local Drug Delivery. J Health Sci Res 2015;6(2):41-46.

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A Systemic Review on the Self Micro Emulsifying Drug Delivery System

International Journal of Pharmaceutical Sciences Review and Research ◽

10.47583/ijpsrr.2021.v69i01.027 ◽

2021 ◽

Vol 69 (1) ◽

Author(s):

Sohansinh Vaghela ◽

Sunita Chaudhary ◽

Ankit Chaudhary

Keyword(s):

Oral Bioavailability ◽

Solid Dispersions ◽

Oral Route ◽

Systemic Review ◽

Intestinal Membrane ◽

Comprehensive Information ◽

First Pass Metabolism ◽

First Pass ◽

Pass Metabolism

Comfort direction and painless method made oral route the most favored. Mainstream of recent active constituents have less oral bioavailability because of dissolution rate limited absorption. While many inventive methods like complexation, cocrystals exist, solid dispersions, pH modification and, lipid-based delivery systems conclusively improved appliance with the seeming rise in drug absorption. Among lipid-based formulations, self-micro emulsifying formulations (SMEDDS) (droplet size < 100 nm) are evident to enhance permeation across intestinal membrane, protection of drug against gastric effect, unit dosage is possible, increased bioavailability of drug, reduces the dose of drug etc. Numerous components are used to formulate these dosage forms like Oil, surfactants, Co-surfactant and lipids mixture contribute to the enhancement in oral bioavailability through promoting the lymphatic passage; thus, hepatic first pass metabolism can be overcoming. The present review highlights comprehensive information on the formulation design, probable mechanisms and characterization of SMEDDS

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