Useful In Vitro Techniques to Evaluate the Mucoadhesive Properties of Hyaluronic Acid-Based Ocular Delivery Systems

Graça, Angélica; Gonçalves, Lídia; Raposo, Sara; Ribeiro, Helena Margarida; Marto, Joana

doi:10.3390/pharmaceutics10030110

Cited by 51 publications

(53 citation statements)

References 30 publications

(47 reference statements)

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Mucoadhesion plays a key role in formulating a successful candidate for ocular delivery [ 39 ]. BSP is proven to be a mucosa protective agent [ 25 ].…”

Section: Discussionmentioning

confidence: 99%

Mucoadhesive Bletilla striata Polysaccharide-Based Artificial Tears to Relieve Symptoms and Inflammation in Rabbit with Dry Eyes Syndrome

et al. 2020

View full text Add to dashboard Cite

Dry eye syndrome (DES) is a multifactorial disorder of the ocular surface affecting many people all over the world. However, there have been many therapeutic advancements for the treatment of DES, substantial long-term treatment remains a challenge. Natural plant-based polysaccharides have gained much importance in the field of tissue engineering for their excellent biocompatibility and unique physical properties. In this study, polysaccharides from a Chinese ground orchid, Bletilla striata, were successfully extracted and incorporated into the artificial tears for DES treatment due to its anti-inflammatory and mucoadhesive properties. The examination for physical properties such as refractive index, pH, viscosity and osmolality of the Bletilla striata polysaccharide (BSP) artificial tears fabricated in this study showed that it was in close association with that of the natural human tears. The reactive oxygen species (ROS) level and inflammatory gene expression tested in human corneal epithelium cells (HCECs) indicated that the low BSP concentrations (0.01–0.1% v/v) could effectively reduce inflammatory cytokines (TNF, IL8) and ROS levels in HCECs, respectively. Longer retention of the BSP-formulated artificial tears on the ocular surface is due to the mucoadhesive nature of BSP allowing lasting lubrication. Additionally, a rabbit’s DES model was created to evaluate the effect of BSP for treating dry eye. Schirmer test results exhibited the effectiveness of 0.1% (v/v) BSP-containing artificial tears in enhancing the tear volume in DES rabbits. This work combines the effectiveness of artificial tears and anti-inflammatory herb extract (BSP) to moisturize ocular surface and to relieve the inflammatory condition in DES rabbit, which further shows great potential of BSP in treating ocular surface diseases like DES in clinics in the future.

show abstract

“…Mucoadhesion plays a key role in formulating a successful candidate for ocular delivery [ 39 ]. BSP is proven to be a mucosa protective agent [ 25 ].…”

Section: Discussionmentioning

confidence: 99%

Mucoadhesive Bletilla striata Polysaccharide-Based Artificial Tears to Relieve Symptoms and Inflammation in Rabbit with Dry Eyes Syndrome

et al. 2020

View full text Add to dashboard Cite

show abstract

“…The mucoadhesion was evaluated by the effect of mucin on zeta potential (ZP) values of Gel A ± mucin (1:1), Gel B ± mucin (1:1). A volume of 40 µL of Gel A, Gel B, and mucin were diluted in either 2 mL of sterile purified water [ 16 , 17 , 18 ]. The ZP values of the different mixtures were measured using a Zetasizer Nanoseries Nano ZS (Malvern Instruments, Malvern, UK) at 35 °C.…”

Section: Methodsmentioning

confidence: 99%

Biopharmaceutical Assessment of Dexamethasone Acetate-Based Hydrogels Combining Hydroxypropyl Cyclodextrins and Polysaccharides for Ocular Delivery

et al. 2020

View full text Add to dashboard Cite

We previously developed two optimized formulations of dexamethasone acetate (DXMa) hydrogels by means of special cubic mixture designs for topical ocular administration. These gels were elaborated with hydroxypropyl-β-CD (HPβCD) and hydroxypropyl-γ-CD (HPγCD) and commercial hydrogels in order to enhance DXMa water solubility and finally DXMa’s ocular bioavailability and transcorneal penetration. The main objective of this study was to characterize them and to evaluate in vitro, ex vivo, and in vivo their safety, biopermanence, and transcorneal permeation. Gels A and B are Newtonian fluids and display a viscosity of 13.2 mPa.s and 18.6 mPa.s, respectively, which increases their ocular retention, according to the in vivo biopermanence study by PET/CT. These hydrogels could act as corneal absorption promoters as they allow a higher transcorneal permeation of DXMa through porcine excised cornea, compared to DEXAFREE® and MAXIDEX®. Cytotoxicity assays showed no cytotoxic effects on human primary corneal epithelial cells (HCE). Furthermore, Gel B is clearly safe for the eye, but the effect of Gel A on the human eye cannot be predicted. Both gels were also stable 12 months at 25 °C after sterilization by filtration. These results demonstrate that the developed formulations present a high potential for the topical ocular administration of dexamethasone acetate.

show abstract

“…The mucoadhesion can be evaluated in vitro by viscosity, rheology, and zeta potential measurements [195]. When using these in vitro methods, not only the method must be chosen but also the mucus substrate.…”

Section: Mucoadhesion Testsmentioning

confidence: 99%

Recent Advances in the Design of Topical Ophthalmic Delivery Systems in the Treatment of Ocular Surface Inflammation and Their Biopharmaceutical Evaluation

et al. 2020

View full text Add to dashboard Cite

Ocular inflammation is one of the most common symptom of eye disorders and diseases. The therapeutic management of this inflammation must be rapid and effective in order to avoid deleterious effects for the eye and the vision. Steroidal (SAID) and non-steroidal (NSAID) anti-inflammatory drugs and immunosuppressive agents have been shown to be effective in treating inflammation of the ocular surface of the eye by topical administration. However, it is well established that the anatomical and physiological ocular barriers are limiting factors for drug penetration. In addition, such drugs are generally characterized by a very low aqueous solubility, resulting in low bioavailability as only 1% to 5% of the applied drug permeates the cornea. The present review gives an updated insight on the conventional formulations used in the treatment of ocular inflammation, i.e., ointments, eye drops, solutions, suspensions, gels, and emulsions, based on the commercial products available on the US, European, and French markets. Additionally, sophisticated formulations and innovative ocular drug delivery systems will be discussed. Promising results are presented with micro- and nanoparticulated systems, or combined strategies with polymers and colloidal systems, which offer a synergy in bioavailability and sustained release. Finally, different tools allowing the physical characterization of all these delivery systems, as well as in vitro, ex vivo, and in vivo evaluations, will be considered with regards to the safety, the tolerance, and the efficiency of the drug products.

show abstract

Useful In Vitro Techniques to Evaluate the Mucoadhesive Properties of Hyaluronic Acid-Based Ocular Delivery Systems

Cited by 51 publications

References 30 publications

Mucoadhesive Bletilla striata Polysaccharide-Based Artificial Tears to Relieve Symptoms and Inflammation in Rabbit with Dry Eyes Syndrome

Mucoadhesive Bletilla striata Polysaccharide-Based Artificial Tears to Relieve Symptoms and Inflammation in Rabbit with Dry Eyes Syndrome

Biopharmaceutical Assessment of Dexamethasone Acetate-Based Hydrogels Combining Hydroxypropyl Cyclodextrins and Polysaccharides for Ocular Delivery

Recent Advances in the Design of Topical Ophthalmic Delivery Systems in the Treatment of Ocular Surface Inflammation and Their Biopharmaceutical Evaluation

Contact Info

Product

Resources

About