Comparative Study of the Mucoadhesive Properties of Polymers for Pharmaceutical Use

E.O., Bakhrushina; Анурова, М. Н.; Демина, Н. Б.; Kashperko, A S; Rastopchina, O. V.; Bardakov, A.I.; Krasnyuk, I. I.

doi:10.3889/oamjms.2020.4930

Cited by 15 publications

(5 citation statements)

References 9 publications

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“…Мукоадгезию изучали по методике определения силы адгезии in vitro, описанной в работе [10]. В ходе эксперимента был использован муцин свиного желудка II типа (SIGMA, Sigma-Aldrich, USA), из которого при тщательном перемешивании с водой в соотношении 1 : 5 до однородного состояния получали 20%-й раствор муцина.…”

Section: фармацевтическая технология Pharmaceutical Technologyunclassified

Development of Ocular Inserts Based on Import Substituted Poloxamer Emuxol 268

Bakhrushina,

Turaeva,

Zhalyalova

et al. 2024

Razrabotka i registraciâ lekarstvennyh sredstv

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Introduction. Emuxol-268 (JSC "NIOPIK", Russia) is a block copolymer produced in Russia with similar in physicochemical and biological properties to poloxamer Kolliphor® P 188 (Pluronic F68) manufactured by BASF, USA. However, a comparison of the properties of natural polymers to assess the prospects of their dosage forms has not been carried out before.Aim. The aim of the study was to demonstrate the interchangeability of auxiliary components using the example of the development of an ophthalmic drug insert by comparing the results of testing the dosage form in terms of such quality parameters as elasticity, thickness, mucoadhesion, pH, biodegradation time and irritation test (hen’s egg-chorioallantoic membrane test, HET-CAM test).Materials and methods. Poloxamers Emuxol 268 (JSC "NIOPIK", Russia) and Kolliphor® P 188 (BASF, Germany), hydroxyethyl cellulose (Natrosol™ 250 HHX, Ashland Global Holdings Inc., USA), and glycerol (LLC "Tulskaya Pharmfabrika", Russia) were used in the experiment. Elasticity, thickness, mucoadhesion, pH, biodegradation time, HET-CAM test were used as screening methods to identify the benefits of the composition.Results and discussion. Experiment results proved that the use of a domestic analogue makes it possible to create an ocular insert with improved quality parameters. The difference in the elasticity index of the inserts differs by 1.3 times, mucoadhesion – 1.7 times, biodegradation time – 2.5 times. In this connection, it can be assumed that an insert based on a domestic polymer contributes to an increase in the time of contact with the eye surface, thereby providing a prolonged effect of the drug and improving its bioavailability. The results obtained may be due to the difference in the average molecular weight of the hydrophobic polyoxypropylene part, which is 2600 Da for Emuxol 268 and 1800 Da for Kolliphor 188. The HET-CAM method showed the same results of the two compositions, both compositions do not have an irritating effect.Conclusion. Summing up, the only analogue of Kolliphor® P 188 available on the Russian pharmaceutical market – Emuxol-268 of JSC NIOPIK is a promising substance for replacement in the development of ophthalmic dosage forms. Despite the differences in physicochemical properties of the domestic block copolymer in comparison with the replaced poloxamer 188, its introduction into placebo inserts gave improved results in terms of quality indicators, which was revealed during a biopharmaceutical analysis.

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Section: фармацевтическая технология Pharmaceutical Technologyunclassified

Development of Ocular Inserts Based on Import Substituted Poloxamer Emuxol 268

Bakhrushina,

Turaeva,

Zhalyalova

et al. 2024

Razrabotka i registraciâ lekarstvennyh sredstv

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“…List of the most common mucoadhesive and water-repellent polymers used to create buccal and sublingual tablets and films. The references related to the properties of the materials are the following [106,[122][123][124][125][126][127][128][129][130][131][132][133][134][135][136][137][138][139]. The column labeled "ref" identifies the previous literature, including creating a tablet or a film with the related material.…”

Section: Concept For Buccal Tablets For the Buccal Delivery Of Nanopa...mentioning

confidence: 99%

Concept for a Unidirectional Release Mucoadhesive Buccal Tablet for Oral Delivery of Antidiabetic Peptide Drugs Such as Insulin, Glucagon-like Peptide 1 (GLP-1), and their Analogs

Pratap-Singh,

Guo,

Baldelli

et al. 2023

Pharmaceutics

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Injectable peptides such as insulin, glucagon-like peptide 1 (GLP-1), and their agonists are being increasingly used for the treatment of diabetes. Currently, the most common route of administration is injection, which is linked to patient discomfort as well as being subjected to refrigerated storage and the requirement for efficient supply chain logistics. Buccal and sublingual routes are recognized as valid alternatives due to their high accessibility and easy administration. However, there can be several challenges, such as peptide selection, drug encapsulation, and delivery system design, which are linked to the enhancement of drug efficacy and efficiency. By using hydrophobic polymers that do not dissolve in saliva, and by using neutral or positively charged nanoparticles that show better adhesion to the negative charges generated by the sialic acid in the mucus, researchers have attempted to improve drug efficiency and efficacy in buccal delivery. Furthermore, unidirectional films and tablets seem to show the highest bioavailability as compared to sprays and other buccal delivery vehicles. This advantageous attribute can be attributed to their capability to mitigate the impact of saliva and inadvertent gastrointestinal enzymatic digestion, thereby minimizing drug loss. This is especially pertinent as these formulations ensure a more directed drug delivery trajectory, leading to heightened therapeutic outcomes. This communication describes the current state of the art with respect to the creation of nanoparticles containing peptides such as insulin, glucagon-like peptide 1 (GLP-1), and their agonists, and theorizes the production of mucoadhesive unidirectional release buccal tablets or films. Such an approach is more patient-friendly and can improve the lives of millions of diabetics around the world; in addition, these shelf-stable formulations ena a more environmentally friendly and sustainable supply chain network.

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“…The differences in mucoadhesive characteristics can be attributed to the swelling and viscosity of polymers [39]. HPMC has a more complex structure than HPC, potentially contributing to superior mucoadhesive properties due to its higher viscosity, facilitating stronger interactions with the mucosal surface [39][40][41]. The presence of hydroxypropyl and methoxyl groups alone increases the polymer's hydrophilicity with a hydrophobic group.…”

Section: Evaluation Of Mucoadhesive Sublingual Tabletsmentioning

confidence: 99%

“…The presence of hydroxypropyl and methoxyl groups alone increases the polymer's hydrophilicity with a hydrophobic group. This structure allows for the formation of hydrophobic interactions in addition to fast wetting and spreading that promote the entanglement of polymer chains upon contact with the mucin surface [40]. Additionally, HPMC possesses the ability to hold fluid within its structure through pores, forming a hydrogel that enhances its ability to form hydrogen bonds with mucin, the major component of mucus.…”

Section: Evaluation Of Mucoadhesive Sublingual Tabletsmentioning

confidence: 99%

The Preparation and Evaluation of Cyanocobalamin Mucoadhesive Sublingual Tablets

Ma’ali,

Naseef,

Qurt

et al. 2023

Pharmaceuticals

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Cobalamin (vitamin B12), an essential vitamin with low oral bioavailability, plays a vital role in cellular functions. This research aimed to enhance the absorption of vitamin B12 using sublingual mucoadhesive tablets by increasing the residence time of the drug at the administration site. This research involved the preparation of different 50 mg placebo formulas using different methods. Formulas with disintegration times less than one minute and appropriate physical characteristics were incorporated into 1 mg of cyanocobalamin (S1–S20) using the direct compression method. The tablets obtained were evaluated ex vivo for residence time, and only those remaining for >15 min were included. The final formulas (S5, S8, S11, and S20) were evaluated in several ways, including pre- and post-compression, drug content, mucoadhesive strength, dissolution, and Permeapad® permeation test employed in the Franz diffusion cell. After conducting the evaluation, formula S11 (Eudragit L100-55) emerged as the most favorable formulation. It exhibited a mucoadhesive residence time of 118.2 ± 2.89 min, required a detachment force of 26 ± 1 g, maintained a drug content of 99.124 ± 0.001699%, and achieved a 76.85% drug release over 22 h, fitting well with the Peppas–Sahlin kinetic model (R2: 0.9949). This suggests that the drug release process encompasses the Fickian and non-Fickian kinetic mechanisms. Furthermore, Eudragit L100-55 demonstrated the highest permeability, boasting a flux value of 6.387 ± 1.860 µg/h/cm2; over 6 h. These findings indicate that including this polymer in the formulation leads to an improved residence time, which positively impacts bioavailability.

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Comparative Study of the Mucoadhesive Properties of Polymers for Pharmaceutical Use

Cited by 15 publications

References 9 publications

Development of Ocular Inserts Based on Import Substituted Poloxamer Emuxol 268

Development of Ocular Inserts Based on Import Substituted Poloxamer Emuxol 268

Concept for a Unidirectional Release Mucoadhesive Buccal Tablet for Oral Delivery of Antidiabetic Peptide Drugs Such as Insulin, Glucagon-like Peptide 1 (GLP-1), and their Analogs

The Preparation and Evaluation of Cyanocobalamin Mucoadhesive Sublingual Tablets

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