Proliposomes as a drug delivery system to decrease the hepatic first-pass metabolism: Case study using a model drug

2014 ◽  
Vol 64 ◽  
pp. 26-36 ◽  
Author(s):  
Sarala Yanamandra ◽  
Natarajan Venkatesan ◽  
Veeran Gowda Kadajji ◽  
Zhijun Wang ◽  
Manish Issar ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
First Pass Metabolism ◽  
First Pass ◽  
Model Drug ◽  
Pass Metabolism

An Insight into delivery of drug through The Skin: Transdermal Drug Delivery system

2021 ◽  
pp. 4-12
Author(s):  
Lakshmi Usha Ayalasomayajula ◽  
M. Kusuma Kumari ◽  
Radha Rani Earle
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Transdermal Drug Delivery ◽  
Drug Delivery Systems ◽  
Dosage Forms ◽  
Transdermal Drug Delivery System ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

In the recent days about 75% of the drugs taken orally are does not show the desired therapeutic effect. Oral conventional dosage forms have several disadvantages such as poor bioavailability due to hepatic first pass metabolism and tendency to produce rapid blood level spikes (Both high and low). Thus, rapid drug levels in the plasma leads to a need of high and/or frequent dosing, which can be both uneconomical and inconvenient. To overcome such disadvantages transdermal drug delivery system was developed. TDDS is such a delivery system which has been explored extensively over the last two decades, with therapeutic success. Transdermal drug delivery systems (TDDS) are the drug delivery systems which involves transportation of drug to epidermal and dermal tissues of the skin for local therapeutic action while major fraction of the drug is transported into the systemic blood circulation. Topical administration of therapeutic agents offers vast advantages over conventional oral and invasive methods of drug delivery. Some of the advantages of transdermal drug delivery include limitation of hepatic first pass metabolism, enhancement of therapeutic efficiency and maintenance of steady state plasma level concentration of the drug. This study includes a brief overview of TDDS, its advantages over conventional dosage forms, drug delivery routes across human skin, permeation enhancers, and classification, formulation, methods of preparation and evaluation of transdermal patches.

Formulation and Characterization of Eplerenone Mucoadhesive Buccal Tablets

2021 ◽  
pp. 3097-3103
Author(s):  
Harini Amballa ◽  
Navaneetha Kaluva ◽  
Sree Giri Prasad Beri ◽  
Krishna Mohan Chinnala ◽  
Mayuri Konda
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Release System ◽  
First Pass Metabolism ◽  
First Pass ◽  
Buccal Tablets ◽  
Pass Metabolism

Mucoadhesive drug release system is a preferably unidirectional release system where mucosal epithelial exterior is enclosed by the mucus deposit that interacts with the bio-adhesive drug delivery system and swelling time of the buccal dosage form which is amplified by mucin molecules at the location of administration. Eplerenone is an Anti-hypertensive drug that undergoes hepatic first pass metabolism and shows 69% of bioavailability. In order to bypass the hepatic first pass metabolism the drug is designed to be delivered through buccal cavity to avoid the first pass metabolism. Eplerenone buccal tablets were formulated by using direct compression method with different polymers like HPMC K 100M, Carbopol 934P, Carbopol 974P, Xantham Gum, Eudragit L100 and NaCMC in various concentrations and compositions. Incompatibility complications were not observed from the FTIR spectrums. The formulated and prepared buccal solid dosage forms were evaluated for pre-compressions and post- compression parameters such as hardness, weight variation, thickness, friability, surface pH, swelling index, in-vitro dissolution studies, drug content uniformity, mucoadhesion strength and mucoadhesion time. Evaluation results of formulation F12 are proven to be the optimal formulation showing highest mucoadhesion time, mucoadhesion strength and in-vitro drug release for prolonged period of time about 8 hours. Eplerenone is best delivered through buccal drug delivery system to enhance its oral bioavailability and bypass the hepatic first pass metabolism.

scholarly journals Development and evaluation of buccal patches of theophylline

2021 ◽  
Vol 16 (3) ◽  
pp. 235-240
Author(s):  
Kapil Kumar ◽  
Gurleen Kaur ◽  
Seema ◽  
Deepak Teotia ◽  
Ikram
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Buccal Mucosa ◽  
Systemic Circulation ◽  
Pharmacological Response ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Buccal patches are the types of formulations in which the drug is administered through buccal mucosa. these patches are or placed in between the gums and the for the pharmacological response. The main advantage of these patches is there is no first pass metabolism takes place and easily absorb in systemic circulation through themucosa .the main objective of this drug delivery system is to elevate or increase the bioavailability of the drug. the review informs about the steps involve in the preparation of buccal patch and to promote the awareness towards this type of drug delivery system. This article intends to analyze the overall profile of Buccal Patches and scope of future advances.

scholarly journals A Brief Review on Bucco-adhesive Drug Delivery System

2021 ◽  
Vol 11 (4-S) ◽  
pp. 231-235
Author(s):  
Sabnam Gupta ◽  
Sudip Das ◽  
Abhay Singh ◽  
Suman Ghosh
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Current Status ◽  
Oral Drug ◽  
Adhesive Systems ◽  
First Pass Metabolism ◽  
First Pass ◽  
Bioadhesive Polymers ◽  
Pass Metabolism

The buccal region within the mucosal cavity of the mouth provides an alternative route over an oral drug administration for systemic as well as local drug delivery. As the buccal mucosa has an abundant blood supply and is relatively permeable, it can be considered as most accessible and desired location for both local and systemic drug delivery. The buccal method for medication delivery greatly helps in avoiding issues in the gastrointestinal environment, such as increased first-pass metabolism and medication degradation. Bucco-adhesive systems offer varieties of advantages such as convenience in administration and termination of therapy in case of emergency, higher patient compliance, better bioavailability, rapid absorption, etc. This current review highlights the bucco-adhesive drug delivery system, its advantages and limitations, mechanisms and theories of mucoadhesion, different bucco-adhesive dosage forms, and bioadhesive polymers. It also highlights the current status on mucoadhesive drug delivery methods for the buccal cavity or bucco-adhesive systems. Keywords: Bioadhesion, mucoadhesion, bucco-adhesive drug delivery system, oral mucosa, first-pass metabolism, bioadhesive polymers.

scholarly journals Sublingual spray: a new technology oriented formulation with multiple benefits

2019 ◽  
Vol 10 (4) ◽  
pp. 2875-2885 ◽  
Author(s):  
Aravindhanthan V ◽  
Anjali P B ◽  
Arun Radhakrishnan
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
New Technology ◽  
Rapid Onset ◽  
Regulatory Agencies ◽  
Onset Of Action ◽  
First Pass ◽  
Delivery Technology ◽  
Pass Metabolism

Sublingual drug delivery system was a well-established platform for delivering the drug that need to exhibit quick action without any first-pass metabolic effect, but various pitfall in the regular sublingual drug delivery systems such as a tablet, capsule etc., that can be overcome by novel sublingual drug delivery technology such as particulate sublingual spray. Sublingual spray for drug administration has gained attention in the market since it proved its propensity to by-pass the first-pass metabolism and to initiate a rapid onset of action due to its atomized micro particulate nature, which is significantly higher than the other sublingual formulations. The approval of sublingual spray by the regulatory agencies may commence further research in this field by subsuming various essential drugs for indications such as cancer pain, cardiovascular issue etc. This article comprises a detailed study on the drawback of conventional sublingual drug delivery system and the approach by which these drawbacks can be overruled by spray technology in the sublingual area and the, in-depth mechanism of drug delivery through sublingual with the help of atomization followed by the entire formulation strategy along with evaluation and industrial perspective of the sublingual spray dosage form as a future tool of patient-friendly drug delivery.

scholarly journals Virosomes as drug delivery system: An updated review

2021 ◽  
Vol 12 (3) ◽  
pp. 2239-2247
Author(s):  
Mohd Muaz Mughees ◽  
Mughees Ahmad Ansari ◽  
Afifa Mughees ◽  
Faisal Farooque ◽  
Mohd Wasi
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Empty Space ◽  
Viral Envelope ◽  
Administration Routes ◽  
B Virus ◽  
First Pass Metabolism ◽  
Almost All ◽  
Pass Metabolism

Amid the era of development in all sphere of Biotechnology, Biochemistry and Pharmacology, it would not be an exaggeration to say that we have a myriad of molecules available to us in labs with promising results against many diseases. The limitation lies in the fact that some molecules are toxic when they act on organs other than their targets. Yet others cannot reach their targets in the desired concentration, be it due to easy degradation in the gut or high first-pass metabolism or very short half-life, etc. Thus, to overcome this, we have an alternate drug delivery system, namely Virosomes. The purpose of this review is to understand the drug delivery aspect of the virosomes, its type, structure, method of preparation, mechanism of action, administration routes and the application in the medical field. Virosomes are the regenerated viral envelope having a central empty space that can act as the vehicles for drug delivery. The central empty space can be filled with the desired bioactive molecule. Virosomes are most commonly prepared by using the reconstituted viral envelope of the Influenza virus, but other virus such as Sendai or HVJ, Hepatitis B Virus, HIV, New castle Disease Virus etc., can also be used for the preparation of virosomes. Virosomes has a great potential as the drug delivery system for almost all types of the drugs, and this encourages the researchers and therapeutic industries to enhance their pharmacological profiles, clinical result and stability. 

Development of Microneedle Devices for Drug Delivery

2021 ◽  
Author(s):  
◽  
Olivia Howells
Keyword(s):  
Drug Delivery ◽  
Stratum Corneum ◽  
Drug Formulation ◽  
Therapeutic Drug ◽  
Hydrophobic Barrier ◽  
First Pass Metabolism ◽  
First Pass ◽  
Out Of Plane ◽  
Pass Metabolism ◽  
Hollow Microneedles

There are numerous modes of therapeutic administration, of which oral delivery is the most convenient and conventional as it involves administration of therapeutics in the form of liquids or solid capsules and tablets. However, this mode encounters several challenges, such as chemical processes within the gastrointestinal track and first pass metabolism which subsequently reduce the efficacy of the therapeutic drugs. To overcome these issues, transdermal drug administration in the form of hypodermic needles, topical creams, and transdermal patches have been employed. However, the effect of transdermal administration is limited due the stratum corneum layer of the skin, which acts as a lipophilic and hydrophobic barrier preventing external molecules from entering the skin. Therefore, hypodermic needles are used due to their sharp tip facilitating penetration through the stratum corneum to deposit the drug formulation into the skin, subcutaneous fat, or muscles layers. However, these needles induce needle-phobia and reduce patient compliance due to the complexity with administration and pain associated with injection. Microneedle devices have been developed to avoid these issues and provide enhanced transdermal therapeutic drug delivery in a minimally invasive manner to eliminate the first-pass metabolism and provide a sustained release. Unlike hypodermic needles injection, they do not cause pain and related fear or phobia in individuals, thereby improving compliance to the prescribed dosage regime. Till now different types of microneedles have been fabricated. These include, solid, coated, hollow and dissolvable, where each type has its own advantages and unique properties and designs. In this thesis, two novel methods utilising silicon etching processes, for the fabrication of both out-of-plane and in-plane silicon microneedles are presented. Hollow out-of-plane microneedles are manufactured through deep reactive-ion etching (DRIE) technology. The patented three-step process flow has been developed to produce multiple arrays of sharp bevelled tipped, hollow microneedles which facilitate easy insertion and controlled fluid injection into excised skin samples. The in-plane microneedles have been fabricated from simultaneous wet KOH etching of the front and reverse of (100) orientated silicon wafers. The characteristic 54.7˚ sidewall etch angle was utilised to form a sharp six-sided microneedle tip and hexagonal shaped shaft. Employing this method allowed fabrication of both solid and hollow microneedles with different geometries i.e., widths and heights of several µm, to determine the optimal MN height and width for effective penetration and transdermal drug delivery. All microneedles fabricated during the PhD studentship tenure have been characterised through histology, fluorescent studies, and delivery into ex-vivo porcine and human skin tissue (research ethics committee reference 08/WSE03/55) to demonstrate effective microneedle based transdermal therapeutic drug delivery. The transdermal delivery of insulin and hyaluronic acid has been successfully demonstrated by employing a simple poke and patch application technique, presenting a clinical improvement over traditional application such as creams and ointments.

scholarly journals A comprehensive review on buccal patches

2020 ◽  
Vol 13 (1) ◽  
pp. 130-135
Author(s):  
Seema ◽  
Kapil kumar ◽  
Deepak Teotia
Keyword(s):  
Drug Delivery ◽  
Oral Cavity ◽  
Systemic Circulation ◽  
Drug Formulation ◽  
Delivery Method ◽  
Modern Approach ◽  
Comprehensive Review ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Buccal Patches are the type of drug formulation that has normally a different course of administration through the buccal mucosa for drug delivery. The product is placed between upper gingiva (gums) and cheek to treat local and systemic conditions. Buccal patch have good accessibility to the membranes that line the oral cavity. These patches tend to help drug enter directly into the systemic circulation escaping hepatic first pass metabolism. This type of drug delivery method is considered useful for elevating the bioavailability of drugs. This review is a thorough study to apprehend the procedures involved in assessment of buccal patches and the modern approach towards this type of drug delivery. This article intends to analyze the overall profile of Buccal Patches and scope of future advances.

Model drug delivery system based on nanodiamonds

2011 ◽  
Vol 6 (3-4) ◽  
pp. 256-264 ◽  
Author(s):  
K. V. Purtov ◽  
A. I. Petunin ◽  
A. P. Puzyr ◽  
A. E. Burov ◽  
V. S. Bondar
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Model Drug
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