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Application of Bioresponsive Polymers in Drug Delivery
Published in Deepa H. Patel, Bioresponsive Polymers, 2020
Manisha Lalan, Deepti Jani, Pratiksha Trivedi, Deepa H. Patel
Literature reveals a large number of research studies on thermoresponsive gels for nasal administration. We will present a bird’s eye view on the subject. Poloxamers have been one of the most researched thermoresponsive polymers. In one of the study, Majithiya et al. developed a composite gel based on Poloxamer 407 and Carbopol 934P for sumatriptan succinate in management of migraine. The transition temperatures were below 30°C. The gel showed mucoadhesive characteristics and enhanced permeability and induced no cellular toxicity [52]. Zaki et al. also worked on Polaxamer 407 but with polyethylene glycol and multiple mucoadhesive polymers for metoclopromide. The inclusion of mucoadhesive polymers modified the rheological properties and increased the residence time as evidenced by longer mucociliary transport time. The formulation also ensured a faster Tmax compared to oral solution [53]. Ketorolac tromethamine nasal sprays gave insufficient nasal residence time to limit their applicability. Another study on thermoresponsive hydrogel of Poloxamer 407 and Carrageenan for ketoraolac ensured higher nasal retention in vivo studies (54).
Dermal and Transdermal Drug Delivery Systems
Published in Tapash K. Ghosh, Dermal Drug Delivery, 2020
Kenneth A. Walters, Majella E. Lane
In the mid-2000s, several reports on the skin permeation of sumatriptan and the effects of skin penetration enhancement strategies were reported. Pretreatment of porcine skin with ethanol, polyethylene glycol 600, sorbitan monolaurate, oleic acid, and terpenes limonene and 1,8-cineole produced an increase in sumatriptan flux (Femenía-Font et al., 2005a). The authors then went on to compare these results to data obtained using human skin and established that a linear relationship of flux through porcine and human skin although the flux through pig skin was double that through human skin (Femenía-Font et al., 2006a). It was found that a combination of chemical enhancement using 1-dodecyl-azacycloheptan-2-one (Azone, laurocapram) and iontophoresis (Femenía-Font et al., 2005b) was the most effective strategy to enhance transdermal absorption of sumatriptan through human skin in vitro. Further experiments aimed at developing a bioadhesive film containing sumatriptan demonstrated that diethylene glycol monoethyl ether (Transcutol) and 2-pyrrolidone decreased sumatriptan permeation when they were included in a film. Rendering the film occlusive was found to increase skin permeation (Femenía-Font et al., 2006b). This team achieved greater success with a sumatriptan succinate transdermal delivery system comprising (a) methylcellulose and propylene glycol (as a plasticiser), (b) polyvinyl pyrrolidone and sorbitol, and (c) polyvinyl pyrrolidone-polyvinyl alcohol plus sorbitol. All systems contained 5% Azone and methacrylate copolymer was used as an adhesive. The films were applied to an occlusive backing membrane. When evaluated on pig ear skin the methylcellulose film provided the greatest flux and this was further increased by iontophoresis (Balaguer-Fernández et al., 2008).
Intranasal drug delivery of sumatriptan succinate-loaded polymeric solid lipid nanoparticles for brain targeting
Published in Drug Development and Industrial Pharmacy, 2022
Rakesh Kumar Yadav, Kamal Shah, Hitesh Kumar Dewangan
Sumatriptan succinate (SS), a 5-hydroxytryptaminereceptor (5-HT1B/5-HT1D) agonist, was the first medicine licensed by the US Food and Drug Administration for the treatment of acute migraine in 1991. Its pharmacological action is mediated through vasoconstriction of the meningeal arteries, restriction of neurotransmitter release from neurons in the brain, suppression of nociceptive transmission, and reduction of trigeminal nerve activity. Sumatriptan is hydrophilic in nature and has been observed to pass the BBB to some amount in its basic form. SS is poorly absorbed and passes through a pre-systemic metabolic process. As a result, it has a limited oral bioavailability of roughly 15%. It has a plasma half-life of 1.5 h and an elimination half-life of 2.5 h, respectively [8,9]. The goal of this study was to create solid lipid nanoparticles (SLNPs) containing SS for nasal delivery to the brain. To improve the entrapment efficiency of hydrophilic drugs, a solvent injection approach was adopted and optimized by central composite design (CCD) model. Further, prepared formulation was evaluated for surface morphology, Fourier-transform infrared (FTIR) spectroscopy, in vitro release, histopathology, and brain targeting.
Recent advances in electrospun for drug delivery purpose
Published in Journal of Drug Targeting, 2019
Mengyao Liu, Yanan Zhang, Siyu Sun, Abdur Rauf Khan, Jianbo Ji, Mingshi Yang, Guangxi Zhai
Fast-dissolving drug delivery systems (FD-DDSs) (e.g. sublingual mucosa DDS) have been attracting great interests in the pharmaceutical industry of all time. These delivery systems could dissolve or disintegrate the drugs very fast in the mouth, without any water to help swallowing. It is these properties that greatly enhances drug bioavailability and helps to deliver drug rapidly. In recent years, fast-release electrospun nanofibers like solid dispersion have been developed, with high surface area, high porosity and ability to encapsulate high amount of drugs. In fact, oral fast-dissolving films of good quality were prepared by single-liquid electrospun as sublingual films [41]. Researchers found that thin thickness (121–131µm), terrible folding endurance (6.67 times), rapid dissolution (<150s) and rapid disintegration in simulated saliva solution (320ms) of obtained paracetamol/caffeine-loaded fibre film were suitable to make the oral fast-dissolving film. As a result of folding endurance decreased by increasing drug loading, obtained film could support higher drug concentration (>90%). Importantly, they also testified that poor folding endurance could be suitable for oral fast-dissolving films, which may be owing to their property that it was too brittle to ensure film stability. However, the folding endurances of other oral fast-dissolving films are over 20 times, expressing the potential of electrospun nanofibers. In addition, sumatriptan succinate, naproxen and their salts and hydrophilic polymers (CS, PVA, PCL and polyacrylic acid (PAA)) were selected to form sublingual dosage for FD-DDSs [26] and found that drug released more than 90% within 10min and two different drugs were incorporated in different layers that could not influence the release of the other, possible to combined treatment. In this study, β-cyclodextrin, a kind of cross-linking agents, helped these systems to reduce drug release through creating new form between drug and polymer. It suggested that appropriate excipient could control the drug release to meet clinical needs. Besides, Potrc et al. [37] used PCL and poorly water-soluble drugs (ibuprofen or carvedilol) to develop the oromucosal delivery system. In phosphate buffer, hydrophilic polymer (PVP) helped water-soluble drugs to incorporate in nanofibers with release of incorporated ibuprofen (100% and 70% the incorporated carvedilol in 4h) in higher amounts. As a result of the interaction between the drug and the polymer, different release properties of two drugs are reasonable. It is worth noticing that the above mentioned is single fluid electrospun process, but other processes could realise FD-DDSs as well. For example, Li, et al. [46] formed quercetin-loaded FD-DDSs using coaxial electrospun. In vitro release research showed that the nanofibers mat obtained with core-sheath structure released the drug completely with 1min, improving solubility of poor water-soluble drug. To some extent, electrospun nanofibers with appropriate polymer could help poorly water-soluble drugs to improve their solubility and hence, realising fast release.