Ocular drug delivery systems

Nayak, Kritika; Choudhari, Manisha; Bagul, Swati; Chavan, Tejas; Misra, Manju

doi:10.1016/b978-0-12-819838-4.00006-7

Cited by 7 publications

(11 citation statements)

References 185 publications

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“…BRB, however, prevents drug entry from the blood into the posterior chamber. It comprises retinal capillaries, which include the inner retina barrier and the retinal pigment epithelium cells (RPEs), considered as the outer blood–retinal barrier, respectively [ 13 , 14 ]. The drug permeability across RPEs is easier to determine, but it is hard to quantitate the permeability values of the vascular component of the BRB.…”

Section: Constraints In Ocular Drug Deliverymentioning

confidence: 99%

Drug Delivery Challenges and Current Progress in Nanocarrier-Based Ocular Therapeutic System

Akhter

Ahmad

Alshahrani

et al. 2022

Gels

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Drug instillation via a topical route is preferred since it is desirable and convenient due to the noninvasive and easy drug access to different segments of the eye for the treatment of ocular ailments. The low dose, rapid onset of action, low or no toxicity to the local tissues, and constrained systemic outreach are more prevalent in this route. The majority of ophthalmic preparations in the market are available as conventional eye drops, which rendered <5% of a drug instilled in the eye. The poor drug availability in ocular tissue may be attributed to the physiological barriers associated with the cornea, conjunctiva, lachrymal drainage, tear turnover, blood–retinal barrier, enzymatic drug degradation, and reflex action, thus impeding deeper drug penetration in the ocular cavity, including the posterior segment. The static barriers in the eye are composed of the sclera, cornea, retina, and blood–retinal barrier, whereas the dynamic barriers, referred to as the conjunctival and choroidal blood flow, tear dilution, and lymphatic clearance, critically impact the bioavailability of drugs. To circumvent such barriers, the rational design of the ocular therapeutic system indeed required enriching the drug holding time and the deeper permeation of the drug, which overall improve the bioavailability of the drug in the ocular tissue. This review provides a brief insight into the structural components of the eye as well as the therapeutic challenges and current developments in the arena of the ocular therapeutic system, based on novel drug delivery systems such as nanomicelles, nanoparticles (NPs), nanosuspensions, liposomes, in situ gel, dendrimers, contact lenses, implants, and microneedles. These nanotechnology platforms generously evolved to overwhelm the troubles associated with the physiological barriers in the ocular route. The controlled-drug-formulation-based strategic approach has considerable potential to enrich drug concentration in a specific area of the eye.

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Section: Constraints In Ocular Drug Deliverymentioning

confidence: 99%

Drug Delivery Challenges and Current Progress in Nanocarrier-Based Ocular Therapeutic System

Akhter

Ahmad

Alshahrani

et al. 2022

Gels

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“…These drug delivery systems reduced the toxicity of many drugs by changing the biodistribution pattern 2 . Apart from sustaining, controlling, targeting, and protecting the drugs from gastric and enzymatic degradation these lipid-based drug delivery systems are considered to be safe and efficient thereby they possess excellent applications in the delivery of various drug molecules for the treatment of various ocular 3 , cancer 4 , diabetic 5 , pulmonary 6 and microbial diseases 7 , cartilage regeneration 8 , wound healing , vaccine delivery 10 , and nutraceuticals 11 . Hence in this present context, a literature survey of the past ten years of publications on lipid-based drug delivery systems like Vesosomes, Phytosomes, Solid Lipid Nanoparticles (SLNs), Nanostructured Lipid Carriers (NLCs), and Archaeosomes with updated literature was highlighted & in many cases development was carried out by trial and errorbased methods.…”

Section: Introductionmentioning

confidence: 99%

Insights of Lipid-Based Drug Delivery Systems with an Emphasis on Quality by Design

Battula¹,

Chinthaginjala²,

Telkar³

et al. 2023

Int J Life Sci Pharm Res

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Lipid-based drug delivery systems offer several advantages and have wide solubility, permeation, and bioavailability enhancement applications. This review provides detailed information on the fabrication, application and aspects of QbD of various lipid-based vesicles. Most of the review studies focused on lipid-based vesicles without the QbD aspect. This review article covers all the lipid-based systems in escalating on the method of QbD, which enhances the bioavailability of active pharmaceutical ingredients in different formulation approaches. Among all the different available approaches towards formulation development, lipid-based drug delivery systems (LBDDS) have continually maintained the limelight on themselves. One of the reasons for the popularity of LBDDS is their ability to solve problems with poorly water-soluble drugs and their bioavailability. Several drugs' efficacy was improved by utilizing this type of delivery system. Vesosomes, Phytosomes, Solid Lipid Nanoparticles (SLNs), Nanostructured Lipid Carriers (NLCs), and Archaeosomes are novel lipid-based systems with unique applications in drug delivery. Hence, the present perspective is to review the various LBDDS approaches utilized to enhance the formulations' performance while dissecting the studies systematically to get a clear outline of various LBDD subsystems, their applications, methods of preparation, and the mechanism of drug delivery. In addition to this, the review also focuses on overcoming the lacunas of the past literature by making an attempt to identify Quality target product profile (QTPP), Critical quality attributes (CQAs) and applying them for the statistical design of experiments and continuous strategy by QbD at the same time harnessing their potential in risk assessment. Applying QbD in developing lipid-based drug delivery systems reduces the number of trials and yields a product with in-built quality as it deliberates various critical variables, process parameters, risk assessment, and control strategy in formulation development.

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“…Due to the large surface area and space, the sclera and conjunctiva of the eye are suitable ways to deliver proteins, peptides, and nucleic acids. However, owing to the presence of many blood vessels, the drug enters the systemic blood flow and is away from the eye area . In corneal absorption, the structure of the cornea is a barrier to drug absorption from this area due to the presence of different layers that are different in terms of hydrophilicity and lipophilicity.…”

Section: Introductionmentioning

confidence: 99%

“…In addition, eye support mechanisms such as tear production and blinking decrease the drug’s retention time in the cornea. All these factors cause the corneal and noncorneal absorption of the drug to be significantly reduced …”

Section: Introductionmentioning

confidence: 99%

Cationic Dextran Stearate (Dex-St-GTMAC): Synthesis and Evaluation as Polymeric Micelles for Indomethacin Corneal Penetration

Firozian,

Arabkhani,

Mahboobian

et al. 2023

ACS Omega

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Background Indomethacin as a non-steroidal anti-inflammatory drug (NSAID) is commonly used to treat some ocular inflammatory disorders. Unfortunately, indomethacin is a drug that is poorly soluble in water; therefore, it has low efficacy. An attractive approach is the targeted delivery of indomethacin to the cornea using cationic dextran stearate as a polymeric micelle drug carrier. Methods A dextran stearate-glycidyl trimethylammonium chloride (Dex-St-GTMAC) copolymer was prepared through the reaction of GTMAC, stearoyl chloride, and dextran. Then, Dex-St-GTMAC was characterized by Fourier transform infrared (FT-IR) spectroscopy and 1H NMR spectroscopy. Dex-St-GTMAC forms micelles in the presence of indomethacin. The prepared polymeric micelles were characterized for size, ζ-potential, drug loading, particle morphology, critical micelle concentration, and encapsulation efficiency. To study the irritation potential of the indomethacin-loaded Dex-St-GTMAC, Het-Cam and Draize tests have been performed. Prepared cationic micelles were subjected to the in vitro drug release and ex vivo trans-corneal permeation test. Results The dialysis method was used for the preparation of indomethacin-loaded micelles (10, 20, and 30%). Measurement of the particle size showed a mean diameter of 122.1 and 150.9 nm for the drug-loaded micelles. Scanning electron microscopy (SEM) images showed that the morphology of the particles is spherical. 10% formulation was chosen as the best formulation due to more surface charge and reasonable drug loading. ζ-potential measurement for the 10% drug-containing micelles showed a value of +39.1 mV. Drug loading efficiency and the encapsulation efficiency for 10% drug-containing micelles were 6.36 and 63.61%, respectively. The results of the Het-Cam and Draize tests indicated that the indomethacin-loaded Dex-St-GTMAC formulation had no toxicity to eye tissues. Based on our results, the prepared micelles (indomethacin-loaded Dex-St-GTMAC) exhibited a sustained drug release pattern compared to the control group. Indomethacin penetration from the micelles to the excised bovine cornea was 1.75-fold greater than the control (indomethacin 0.1% in phosphate-buffered saline (PBS)). Conclusions Data from the ζ-potential, SEM, drug loading capacity, and in vitro drug release studies indicated that cationic dextran stearate polymeric micelles are an appropriate carrier for the efficient penetration of indomethacin into cornea tissues.

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Ocular drug delivery systems

Cited by 7 publications

References 185 publications

Drug Delivery Challenges and Current Progress in Nanocarrier-Based Ocular Therapeutic System

Drug Delivery Challenges and Current Progress in Nanocarrier-Based Ocular Therapeutic System

Insights of Lipid-Based Drug Delivery Systems with an Emphasis on Quality by Design

Cationic Dextran Stearate (Dex-St-GTMAC): Synthesis and Evaluation as Polymeric Micelles for Indomethacin Corneal Penetration

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