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

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. 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). 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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Self-assembled liposome from multi-layered fibrous mucoadhesive membrane for buccal delivery of drugs having high first-pass metabolism

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2018.05.062 ◽

2018 ◽

Vol 547 (1-2) ◽

pp. 303-314 ◽

Cited By ~ 14

Author(s):

Jianting Chen ◽

Hao Pan ◽

Yining Yang ◽

Shihang Xiong ◽

Hongliang Duan ◽

...

Keyword(s):

Buccal Delivery ◽

First Pass Metabolism ◽

First Pass ◽

Self Assembled ◽

Pass Metabolism

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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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Optimasi Hidroksipropil Metilselulosa K-4M dan Carbopol® 940 pada Sediaan Patch Dispersi Padat Piroksikam

Kartika Jurnal Ilmiah Farmasi ◽

10.26874/kjif.v5i2.133 ◽

2018 ◽

Vol 5 (2) ◽

pp. 80

Author(s):

Dwi Nurahmanto ◽

Nurul Shalikha ◽

Lidya Ameliana

Keyword(s):

Moisture Content ◽

Solid Dispersion ◽

Hydroxypropyl Methylcellulose ◽

Lattice Design ◽

Simplex Lattice Design ◽

Peg 4000 ◽

First Pass Metabolism ◽

First Pass ◽

Simplex Lattice ◽

Pass Metabolism

Abstrak Piroksikam merupakan anti inflamasi non steroid (AINS) turunan oksikam yang berkhasiat sebagai analgesik dan antiinflamasi digunakan untuk pengobatan rheumatoid arthritis dan osteoarthritis. Piroksikam menyebabkan masalah pada saluran cerna dan first pass metabolism yang dapat dihindari dengan cara pemberian transdermal patch. Salah satu komponen patch yaitu polimer yang berfungsi untuk mengontrol kecepatan pelepasan obat dari sediaan. Penelitian ini dilakukan untuk menentukan komposisi terbaik dari kombinasi polimer hidroksipropil metilselulosa (HPMC) dan Carbopol terhadap % moisture content (MC) dan flux pelepasan sediaan transdermal patch dispersi padat piroksikam dengan rancangan formula Simplex Lattice Design. Piroksikam dibuat dalam bentuk dispersi padat dengan pembawa PEG 4000 untuk meningkatkan kelarutannya. Rancangan formula patch dispersi padat piroksikam dibuat dengan menggunakan tiga polimer Etil selulosa:HPMC:carbopol dimana yang divariasikan adalah perbandingan HPMC : Carbopol yaitu 1 : 0 ; 0,5 : 0,5 ; 0 : 1. Hasil uji menunjukkan ketiga formula memenuhi persyaratan keseragaman kadar dengan rentang keseragaman 3,735 – 97,349 %. Hasil juga menunjukkan formula 3 menghasilkan patch yang lebih tebal, pH permukaan patch lebih rendah, nilai % moisture content lebih besar dan nilai flux lebih tinggi dibandingkan formula 2 dan formula 3, Formula 3 mempunyai nilai % moisture content yang memenuhi persyaratan sebesar 6,613% dan nilai flux pelepasa yang paling bagus sebesar 32,562 µg/cm2.menit1/2. Hasil penelitian juga menunjukkan formula 1 memiliki keseragaman bobot lebih baik dibandingkan formula 2 dan formula 3. Dapat disimpulkan bahwa komposisi optimum dari kombinasi polimer HPMC dan Carbopol pada sediaan patch dispersi padat piroksikam yaitu formula dengan komposisi polimer HPMC sebanyak 0 mg dan Carbopol sebanyak 75 mg. Kata kunci: Dispersi padat, patch piroksikam, HPMC, Carbopol Optimization of Hydroxypropyl Methylcellulose K-4M and Carbopol® 940 in Solid Dispersion Piroxicam Patch Abstract Piroxicam is a non-steroidal anti-inflammatory (NSA) oxysmic derivative as an analgesic and anti-inflammatory agent used for the treatment of rheumatoid arthritis and osteoarthritis. Piroxicam causes problems in the gastrointestinal tract and first pass metabolism that can be avoided by giving transdermal patches. One of the patch components is a polymer that serves to control the speed of drug release from the preparation. The present study was conducted to determine the best composition of the combination of hydroxypropyl methylcellulose (HPMC) and Carbopol polymers against% moisture content (MC) and fluxes release of the pyroxicam dispersion transdermal patch dispersion with the design of the Simplex Lattice Design formula. Piroxicam is prepared in the form of a solid dispersion with a PEG 4000 carrier to increase its solubility. The design of a pyroxicam solid dispersion patch formulation was prepared using three ethyl cellulose polymers: HPMC: carbopol wherein the HPMC ratio is computed: Carbopol is 1: 0; 0.5: 0.5; 0: 1. The test results show the three formulas meet the requirements of uniformity of the content with a uniformity range of 3.735 - 97.349%. the results also show formula 3 resulting in thicker patches, lower patch pH surfaces, greater moisture content values and higher flux values than formula 2 and formula 3, Formula 3 has a moisture content value of 6.613% the finest fl ux flux of 32,562 μg / cm2.menit1 / 2. The results also show that formula 1 has better weight uniformity than formula 2 and formula 3. It can be concluded that the optimum composition of HPMC and Carbopol polymer combinations in the preparation of piroxicam solid dispersion patch is a formula with HPMC polymer composition as 0 mg and Carbopol as much as 75 mg.. Key words: solid dispersion, piroxicam patch, HPMC, Carbopol

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Optimasi Hidroksipropil Metilselulosa K-4M dan Carbopol® 940 pada Sediaan Patch Dispersi Padat Piroksikam

Kartika Jurnal Ilmiah Farmasi ◽

10.26874/kjif.v5i2.121 ◽

2017 ◽

Vol 5 (2) ◽

pp. 80

Author(s):

Dwi Nurahmanto ◽

Nurul Shalikha ◽

Lidya Ameliana

Keyword(s):

Moisture Content ◽

Solid Dispersion ◽

Hydroxypropyl Methylcellulose ◽

Lattice Design ◽

Simplex Lattice Design ◽

Peg 4000 ◽

First Pass Metabolism ◽

First Pass ◽

Simplex Lattice ◽

Pass Metabolism

Abstrak Piroksikam merupakan anti inflamasi non steroid (AINS) turunan oksikam yang berkhasiat sebagai analgesik dan antiinflamasi digunakan untuk pengobatan rheumatoid arthritis dan osteoarthritis. Piroksikam menyebabkan masalah pada saluran cerna dan first pass metabolism yang dapat dihindari dengan cara pemberian transdermal patch. Salah satu komponen patch yaitu polimer yang berfungsi untuk mengontrol kecepatan pelepasan obat dari sediaan. Penelitian ini dilakukan untuk menentukan komposisi terbaik dari kombinasi polimer hidroksipropil metilselulosa (HPMC) dan Carbopol terhadap % moisture content (MC) dan flux pelepasan sediaan transdermal patch dispersi padat piroksikam dengan rancangan formula Simplex Lattice Design. Piroksikam dibuat dalam bentuk dispersi padat dengan pembawa PEG 4000 untuk meningkatkan kelarutannya. Rancangan formula patch dispersi padat piroksikam dibuat dengan menggunakan tiga polimer Etil selulosa:HPMC:carbopol dimana yang divariasikan adalah perbandingan HPMC : Carbopol yaitu 1 : 0 ; 0,5 : 0,5 ; 0 : 1. Hasil uji menunjukkan ketiga formula memenuhi persyaratan keseragaman kadar dengan rentang keseragaman 3,735 – 97,349 %. Hasil juga menunjukkan formula 3 menghasilkan patch yang lebih tebal, pH permukaan patch lebih rendah, nilai % moisture content lebih besar dan nilai flux lebih tinggi dibandingkan formula 2 dan formula 3, Formula 3 mempunyai nilai % moisture content yang memenuhi persyaratan sebesar 6,613% dan nilai flux pelepasa yang paling bagus sebesar 32,562 µg/cm2.menit1/2. Hasil penelitian juga menunjukkan formula 1 memiliki keseragaman bobot lebih baik dibandingkan formula 2 dan formula 3. Dapat disimpulkan bahwa komposisi optimum dari kombinasi polimer HPMC dan Carbopol pada sediaan patch dispersi padat piroksikam yaitu formula dengan komposisi polimer HPMC sebanyak 0 mg dan Carbopol sebanyak 75 mg. Kata kunci: Dispersi padat, patch piroksikam, HPMC, Carbopol Optimization of Hydroxypropyl Methylcellulose K-4M and Carbopol® 940 in Solid Dispersion Piroxicam Patch Abstract Piroxicam is a non-steroidal anti-inflammatory (NSA) oxysmic derivative as an analgesic and anti-inflammatory agent used for the treatment of rheumatoid arthritis and osteoarthritis. Piroxicam causes problems in the gastrointestinal tract and first pass metabolism that can be avoided by giving transdermal patches. One of the patch components is a polymer that serves to control the speed of drug release from the preparation. The present study was conducted to determine the best composition of the combination of hydroxypropyl methylcellulose (HPMC) and Carbopol polymers against% moisture content (MC) and fluxes release of the pyroxicam dispersion transdermal patch dispersion with the design of the Simplex Lattice Design formula. Piroxicam is prepared in the form of a solid dispersion with a PEG 4000 carrier to increase its solubility. The design of a pyroxicam solid dispersion patch formulation was prepared using three ethyl cellulose polymers: HPMC: carbopol wherein the HPMC ratio is computed: Carbopol is 1: 0; 0.5: 0.5; 0: 1. The test results show the three formulas meet the requirements of uniformity of the content with a uniformity range of 3.735 - 97.349%. the results also show formula 3 resulting in thicker patches, lower patch pH surfaces, greater moisture content values and higher flux values than formula 2 and formula 3, Formula 3 has a moisture content value of 6.613% the finest fl ux flux of 32,562 μg / cm2.menit1 / 2. The results also show that formula 1 has better weight uniformity than formula 2 and formula 3. It can be concluded that the optimum composition of HPMC and Carbopol polymer combinations in the preparation of piroxicam solid dispersion patch is a formula with HPMC polymer composition as 0 mg and Carbopol as much as 75 mg.. Key words: solid dispersion, piroxicam patch, HPMC, Carbopol

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Design, Development and Characterization of Nifedipine Microspheres

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v9i3.2627 ◽

2019 ◽

Vol 9 (3) ◽

pp. 138-146

Author(s):

Arun Kumar Chalamalasetty ◽

Boggula Narender ◽

Bolledla Nirosha ◽

Bakshi Vasudha ◽

Peddapalli Himabindu

Keyword(s):

Particle Size ◽

Drug Release ◽

Oral Bioavailability ◽

Ethyl Cellulose ◽

Hydroxypropyl Methylcellulose ◽

Prolonged Release ◽

Design Development ◽

First Pass Metabolism ◽

First Pass ◽

Pass Metabolism

Back ground: Nifedipine is a calcium channel blocker and is used in treatment of angina of angina pectoris and hypertension. Nifedipine readily and almost completely absorbed from GIT, but undergoes first pass metabolism, resulting in low oral bioavailability is about 50%. Aim: The aim of the present study was to prepare and evaluate the microspheres of nifedipine with a goal of improving the bioavailability and giving a prolonged release of drug. Method: Emulsification (o/w) solvent evaporation method was employed in the preparation of nifedipine microparticles using ethyl cellulose and combination of ethyl cellulose and hydroxypropyl methylcellulose as the polymers. Results: FT-IR spectra of physical mixture showed no significant shifting of the peaks therefore it reveals that the drug is compatible with the polymer used. The percentage yield obtained in all the formulations was good and in the range of 59.25-94.44%. Among all the formulations, formulation with combination of ethyl cellulose and hydroxypropyl methylcellulose polymers M9 showed high amount of drug release i.e. (91.23%) in 12hrs. Drug release from microspheres with small mean particle size was faster than those with large mesh particle size and followed Higuchi model of kinetics. Conclusion: The obtained results could be used as essence to develop microspheres, which bypasses first-pass metabolism and results in the improvement of bioavailability. Hence, the present study has been a satisfactory attempt to formulate microspheres of nifedipine, with a view of improving its oral bioavailability and giving a prolonged release of drug. Keywords: Microspheres, nifedipine, hydroxypropyl methylcellulose E5, ethyl cellulose.

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Parenteral systems for statin delivery: a review

Lipids in Health and Disease ◽

10.1186/s12944-019-1139-8 ◽

2019 ◽

Vol 18 (1) ◽

Cited By ~ 3

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.

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