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.

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.

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.

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

scholarly journals FORMULATION, IN VITRO AND EX VIVO CHARACTERIZATION OF MUCOADHESIVE BUCCAL TABLETS FOR ANTIHYPERTENSIVE DRUG

2018 ◽  
Vol 11 (8) ◽  
pp. 402 ◽  
Author(s):  
Himabindu Peddapalli ◽  
Vasudha Bakshi ◽  
Narender Boggula
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Surface Ph ◽  
Ex Vivo Permeation ◽  
First Pass Metabolism ◽  
First Pass ◽  
Permeation Studies ◽  
Buccal Tablets ◽  
Pass Metabolism

Objective: Olmesartan belongs to a class of angiotensin II receptor blockers. It is used in the treatment of hypertension. However, it undergoes extensive hepatic first-pass metabolism, resulting in low oral bioavailability is about 26%. The aim of this study was to prepare and evaluate the mucoadhesive buccal tablets of olmesartan with a goal to increase the bioavailability and improve the patient compliance.Methods: Mucoadhesive buccal tablets were prepared by a direct compression technique using mucoadhesive polymers such as hydroxypropyl methylcellulose (HPMC K4M), sodium carboxymethylcellulose (SCMC), and Carbopol 934P. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, swelling index, drug content uniformity, in vitro drug release, ex vivo mucoadhesive strength, ex vivo mucoadhesive time, and ex vivo permeation studies. The release kinetics was calculated to determine the drug release mechanism. Results: The physicochemical properties of all the formulations were shown to be within the limits. The optimized buccal tablets F2, F7, and F11 showed satisfactory drug release rates with the diffusion controlled mechanism. Optimized buccal tablets developed for olmesartan possess reasonable mucoadhesive strength, mucoadhesive time, and surface pH was in an acceptable salivary pH 6.76±0.28–6.89±0.34. The ex vivo permeation studies for optimized tablets were shown satisfactory drug permeation and could meet the target flux 0.991 mg h−1cm−2.Conclusion: The obtained results could be used as a platform to develop the buccal delivery of this drug, which bypasses the first-pass metabolism and results in the improvement of bioavailability. Hence, the present study concludes that the olmesartan could be delivered through the buccal route.

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.

In Vitro and In Vivo Drug Release from a Novel In Situ Forming Drug Delivery System

2007 ◽  
Vol 25 (6) ◽  
pp. 1347-1354 ◽  
Author(s):  
Heiko Kranz ◽  
Erol Yilmaz ◽  
Gayle A. Brazeau ◽  
Roland Bodmeier
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Situ Forming

Formulation and Evaluation of Solid Self-Nanoemulsifying Drug Delivery System for Enhancing the Solubility and Dissolution Rate of Budesonide

2021 ◽  
pp. 5755-5763
Author(s):  
Kanuri Lakshmi Prasad ◽  
Kuralla Hari
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
Water Soluble ◽  
Drug Release Profile ◽  
Water Soluble Drug

Objective: To enhance solubility and dissolution rate of budesonide through development of solid self-nanoemulsifying drug delivery system (S-SNEDDS). Methods: Liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) were prepared and ternary phase diagram was constructed using Origin pro 8. Liquid self-nanoemulsifying formulation LF2 having 20% oil and 80% of surfactant/co-surfactant was optimized from the three formulations (LF1-LF3) to convert in to solid, through various characterization techniques like self-emulsification, in vitro drug release profile and drug content estimation. The prepared L-SNEDDS converted into S-SNEDDS, SF1-SF6 by adsorption technique using Aerosil 200, Neusilin US2, and Neusilin UFL2 to improve flowability, compressibility and stability. Results: Formulation LF2 exhibited globule size of 82.4 nm, PDI 0.349 and Zeta potential -28.6 mV with drug indicating the stability and homogeneity of particles. The optimized formulation SF4 containing Neusilin UFL2 was characterized by DSC, FTIR, X-Ray diffraction studies and found no incompatibility and no major shifts were noticed. Formulation SF4 released 100 % drug in 20 min against pure drug release of 47 % in 60 min. Regardless of the form (i.e. liquid or solid) similar performance of emulsification efficiency is observed. Conclusion: The results demonstrated that the technique of novel solid self-nanoemulsifying drug delivery system can be employed to enhance the solubility and dissolution rate of poorly water-soluble drug budesonide.

Schiff base-containing dextran nanogel as pH-sensitive drug delivery system of doxorubicin: Synthesis and characterization

2018 ◽  
Vol 33 (2) ◽  
pp. 170-181 ◽  
Author(s):  
Hongying Su ◽  
Wen Zhang ◽  
Yayun Wu ◽  
Xiaodong Han ◽  
Gang Liu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Schiff Base ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ph Sensitive ◽  
Cell Uptake ◽  
Stimuli Responsive ◽  
Drug Release Profile

Stimuli-responsive hydrogels have been widely researched as carrier systems, due to their excellent biocompatibility and responsiveness to external physiologic environment factors. In this study, dextran-based nanogel with covalently conjugated doxorubicin (DOX) was developed via Schiff base formation using the inverse microemulsion technique. Since the Schiff base linkages are acid-sensitive, drug release profile of the DOX-loaded nanogel would be pH-dependent. In vitro drug release studies confirmed that DOX was released much faster under acidic condition (pH 2.0, 5.0) than that at pH 7.4. Approximately 66, 28, and 9% of drug was released in 72 h at pH 2.0, 5.0, and 7.4, respectively. Cell uptake by the human breast cancer cell (MCF-7) demonstrated that the DOX-loaded dextran nanogel could be internalized through endocytosis and distributed in endocytic compartments inside tumor cells. These results indicated that the Schiff base-containing nanogel can serve as a pH-sensitive drug delivery system. And the presence of multiple aldehyde groups on the nanogel are available for further conjugations of targeting ligands or imaging probes.

A Smart Drug Delivery System Based on Thermo-Responsive Polymer Gated Au NRs@SiO2 Nano-Platform

2021 ◽  
Vol 16 (7) ◽  
pp. 1029-1036
Author(s):  
Hongzhu Wang ◽  
Mengxun Chen ◽  
Liping Song ◽  
Youju Huang
Keyword(s):  
Drug Delivery ◽  
Block Copolymer ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Photothermal Therapy ◽  
Drug Loading ◽  
Temperature Sensitive

A key challenge for nanoparticles-based drug delivery system is to achieve manageable drug release in tumour cell. In this study, a versatile system combining photothermal therapy and controllable drug release for tumour cells using temperature-sensitive block copolymer coupled Au NRs@SiO2 is reported. While the Au NRs serve as hyperthermal agent and the mesoporous silica was used to improve the drug loading and decrease biotoxicity. The block copolymer acted as “gatekeeper” to regulate the release of model drug (Doxorubicin hydrochloride, DOX). Through in vivo and in vitro experiments, we achieved the truly controllable drug release and photothermal therapy with the collaborative effect of the three constituents of the nanocomposites. The reported nanocomposites pave the way to high-performance controllable drug release and photothermal therapy system.

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