Development, Characterization, and Ex Vivo Assessment of Elastic Liposomes for Enhancing the Buccal Delivery of Insulin

Bashyal, Santosh; Seo, Jeong-Sun; Keum, Taekwang; Noh, Gyubin; Lamichhane, Shrawani; Lee, Sang Kil

doi:10.3390/pharmaceutics13040565

Cited by 28 publications

(12 citation statements)

References 45 publications

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“…Lyophilization presents a great potential in the pharmaceutical field not only as a technique for the preservation of thermolabile drugs, but also as a technological process for developing drug delivery systems based on nanoparticles. This technique produces oral disintegrating tablets and has been recently applied to produce a mucoadhesive matrix and wafers for buccal drug delivery [ 26 , 27 , 28 ]. The advantages of the sublingual cavity for systemic drug absorption combined with the benefits of liposomes as drug carriers are a promising opportunity for developing innovative pharmaceutical formulations with application to new and old drugs.…”

Section: Introductionmentioning

confidence: 99%

Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

et al. 2022

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A pharmaceutical vehicle based on lyophilized liposomes is proposed for the buccal administration of drugs aimed at systemic delivery through the sublingual mucosa. Liposomes made of egg phosphatidylcholine and cholesterol (7/3 molar ratio) were prepared and lyophilized in the presence of different additive mixtures with mucoadhesive and taste-masking properties. Palatability was assayed on healthy volunteers. The lyophilization cycle was optimized, and the lyophilized product was compressed to obtain round and capsule-shaped tables that were evaluated in healthy volunteers. Tablets were also assayed regarding weight and thickness uniformities, swelling index and liposome release. The results proved that lyophilized liposomes in unidirectional round tablets have palatability, small size, comfortability and buccal retention adequate for sublingual administration. In contact with water fluids, the tablets swelled, and rehydrated liposomes were released at a slower rate than permeation efficiency determined using a biomimetic membrane. Permeability efficiency values of 0.72 ± 0.34 µg/cm2/min and 4.18 ± 0.95 µg/cm2/min were obtained for the liposomes with and without additives, respectively. Altogether, the results point to the vehicle proposed as a liposomal formulation suitable for systemic drug delivery through the sublingual mucosa.

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Section: Introductionmentioning

confidence: 99%

Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

et al. 2022

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“…Ex vivo studies were performed to evaluate the distribution of HIP-nanocomplexes across porcine buccal tissue using a vertical static Franz diffusion cell by using the procedure reported previously. 36 Briefly, the Franz diffusion cell system was set up as described earlier, and 500 µL of FITC-insulin solution, FITC-C1, or FITC-C2 (equivalent to 200 µg/mL FITC–insulin) was loaded into the donor chamber. The studies were directed from the donor to receptor chambers with constant magnetic stirring (600 rpm) at 37°C, and at predetermined time points (0.5, 2, and 4 h), the buccal tissues were washed with PBS buffer (pH 7.4) and dried with soft paper.…”

Section: Methodsmentioning

confidence: 99%

Facilitated Buccal Insulin Delivery via Hydrophobic Ion-Pairing Approach: In vitro and ex vivo Evaluation

Bashyal¹,

Seo²,

Keum³

et al. 2021

IJN

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Background:The clinical use of therapeutic peptides has been limited because of their inefficient delivery approaches and, therefore, inadequate delivery to target sites. Buccal administration of therapeutic peptides offers patients a potential alternative to the current invasive routes of administration. Purpose: The aim of the study was to fabricate hydrophobic ion-pairing (HIP)-nanocomplexes (C1 and C2) utilizing anionic bile salts and cationic peptides, and to assess their permeability across TR146 buccal cell layers and porcine buccal tissue. Methods: C1 and C2-nanocomplexes were fabricated using the HIP approach. In addition, their physiochemical and morphological attributes, in vitro and ex vivo permeability properties, and qualitative and quantitative cellular uptake were evaluated and compared. The localization of C1 and C2-nanocomplexes in porcine buccal tissue was determined using confocal laser scanning microscopy. Results: The C1-nanocomplex was the superior nanocarrier and significantly enhanced the transport of insulin across TR146 cell layers and porcine buccal tissue, exhibiting a 3.00-and 51.76-fold increase in permeability coefficient, respectively, when compared with insulin solution (p < 0.01). C1-nanocomplex was more efficient than C2-nanocomplex at facilitating insulin permeability, with a 2.18-and 27.64-fold increase across TR146 cell layers and porcine buccal tissue, respectively. The C1-nanocomplex demonstrated immense uptake and localization of insulin in TR146 cells and porcine buccal tissue, as evidenced by a highly intense fluorescence in TR146 cells, and a great shift of fluorescence intensity towards the inner region of buccal tissue over time. The increase in fluorescence intensity was observed in the order of C1 > C2 > insulin solution. Conclusion:In this study, we highlighted the efficacy of potential nanocarriers in addressing the daunting issues associated with the invasive administration of insulin and indicated a promising strategy for the buccal administration and delivery of this life-saving peptide hormone.

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“…Bashyal et al produced sodium cholate-incorporated elastic liposomes and sodium glycodeoxycholate-incorporated elastic liposomes, which were tested across porcine buccal tissues using confocal laser scanning microscopy [ 76 ]. The authors showed significantly enhanced the permeation of insulin with a 4.33-fold increase in the permeability coefficient compared to insulin solution.…”

Section: Applications Of Ultra-deformable Liposomesmentioning

confidence: 99%

Elastic and Ultradeformable Liposomes for Transdermal Delivery of Active Pharmaceutical Ingredients (APIs)

Souto

Macedo

Dias-Ferreira

et al. 2021

IJMS

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Administration of active pharmaceutical ingredients (APIs) through the skin, by means of topical drug delivery systems, is an advanced therapeutic approach. As the skin is the largest organ of the human body, primarily acting as a natural protective barrier against permeation of xenobiotics, specific strategies to overcome this barrier are needed. Liposomes are nanometric-sized delivery systems composed of phospholipids, which are key components of cell membranes, making liposomes well tolerated and devoid of toxicity. As their lipid compositions are similar to those of the skin, liposomes are used as topical, dermal, and transdermal delivery systems. However, permeation of the first generation of liposomes through the skin posed some limitations; thus, a second generation of liposomes has emerged, overcoming permeability problems. Various mechanisms of permeation/penetration of elastic/ultra-deformable liposomes into the skin have been proposed; however, debate continues on their extent/mechanisms of permeation/penetration. In vivo bioavailability of an API administered in the form of ultra-deformable liposomes is similar to the bioavailability achieved when the same API is administered in the form of a solution by subcutaneous or epi-cutaneous injection, which demonstrates their applicability in transdermal drug delivery.

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Development, Characterization, and Ex Vivo Assessment of Elastic Liposomes for Enhancing the Buccal Delivery of Insulin

Cited by 28 publications

References 45 publications

Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

Facilitated Buccal Insulin Delivery via Hydrophobic Ion-Pairing Approach: In vitro and ex vivo Evaluation

Elastic and Ultradeformable Liposomes for Transdermal Delivery of Active Pharmaceutical Ingredients (APIs)

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