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Fenugreek
Published in Dilip Ghosh, Prasad Thakurdesai, Fenugreek, 2022
Ujjwala Kandekar, Sunil Ramdasi, Prasad Thakurdesai
Beads are spherical particles of size 50 nm to 2 mm, mostly designed for sustained release of drugs. Versatile drug delivery could be attained by the use of a variety of polymers in bead formulation. In recent years, a great deal of attention has been paid to the development of mucoadhesive hydrogel beads using plant-derived mucilages for controlled release drug delivery (Ahmad et al. 2019; Mishra et al. 2021). Many natural polymers exhibited good mucoadhesive properties and are effectively used for the controlled release of the drug in the formulation of beads (Kandekar et al. 2019; Li et al. 2019; Vakili et al. 2019).
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).
Recent Cannabinoid Delivery Systems
Published in Betty Wedman-St Louis, Cannabis as Medicine, 2019
Natascia Bruni, Carlo Della Pepa, Simonetta Oliaro-Bosso, Daniela Gastaldi, Franco Dosio, Enrica Pessione
NLC have recently been proposed for administration as a dosage form for nasal delivery. Nanospheres of 200 nm diameter, composed of either cetyl palmitate or glyceryl dibehenate and loaded with THC, were obtained. In vitro mucoadhesion evaluations have revealed that cationic NLC formulations (obtained via the addition of cetylpyridinium chloride) should have high mucoadhesiveness properties [123]. The solid matrix of the NLC was found to have a stabilizing effect on THC. Indeed, 91% of the THC was unaltered after 6 months storage at 4°C. About 1.7 mg THC is administered with one spray of the 0.25% THC-loaded NLC formulation in each nostril. This amount was close to the THC amounts obtained from the oromucosal formulation in a study by Johnson et al. [124].
Research progress of ophthalmic preparations of immunosuppressants
Published in Drug Delivery, 2023
Ye Liu, Haonan Xu, Na Yan, Zhan Tang, Qiao Wang
Based on CD intrinsic properties, tacrolimus solubility was improved by approximately 42 times (Mahmoudi et al., 2020). The tacrolimus/HPβCD formulations were prepared by dissolving HPβCD and then adding tacrolimus (García-Otero et al., 2021). Nuclear Magnetic Resonance (NMR) and molecular modeling studies have reported that 0.02% tacrolimus concentration could be obtained by using 40% HPβCD aqueous solutions. Results of ex vivo bio adhesion revealed good mucoadhesive properties. Positron emission tomography/computed tomography imaging (PET/CT imaging) was used as a molecular imaging technique to investigate the in vivo formulations’ permanence on the corneal surface. According to the PET/CT studies, the formulations were mucoadhesive and maintained a long-term presence on the ocular surface owing to an adequate consistency. The time of in vivo ocular permanence was higher (t1/2 of 86.2 min for the 40% HPβCD eyedrop and t1/2 of 46.3 min for the reference formulation of 0.03% tacrolimus ointment Prograf®). This novel eye drop formulation offers high potential as a safe alternative and a versatile vehicle to incorporate new topical ophthalmic drugs.
Fabrication and analysis of chitosan oligosaccharide based mucoadhesive patch for oromucosal drug delivery
Published in Drug Development and Industrial Pharmacy, 2022
Ashwini Kumar, Ram Kumar Sahu, Shibu Chameettachal, Falguni Pati, Awanish Kumar
Mucoadhesive polymers and permeation enhancers are the two major constituents that are required for the proper transport of the drug across buccal mucosa. The mucous coat of the salivary pellicle (thin salivary layer on the buccal mucosa; around 50 µm thick) is responsible for interacting with the mucoadhesive polymer in the formulation. The major constituent of this layer is the mucin protein (negatively charged glycoprotein) that imparts viscosity to the saliva [9]. Some common mucoadhesive polymers are chitosan, sodium alginate, carboxymethylcellulose, and polyacrylic acid. Besides their natural forms, modified polymers such as thiolated polymers have also been successfully used as mucoadhesive polymers [9]. Permeation enhancers are natural or synthetic chemicals that enhance the transport of the drug across any mucosal epithelium. These chemicals should be nonirritant, nontoxic, and biocompatible. Permeation enhancers have been characterized as fatty acids (disrupting the intercellular lipids), bile salts (disrupting the membrane fluidity and creating channels), and azones (disrupting membrane lipids). Chitosan is a unique mucoadhesive biopolymer that consists of substantially good permeation-enhancing properties. Chitosan is also reported to reduce the trans-epithelial electrical resistance (TEER) that further facilitates drug permeation [10,11]. Besides being highly mucoadhesive and facilitating permeation, chitosan demonstrates high biocompatibility, and biodegradability, and possesses efflux pump inhibition ability [11].
Current status of the development of intravesical drug delivery systems for the treatment of bladder cancer
Published in Expert Opinion on Drug Delivery, 2020
Ho Yub Yoon, Hee Mang Yang, Chang Hyun Kim, Yoon Tae Goo, Myung Joo Kang, Sangkil Lee, Young Wook Choi
Mucoadhesion/retention is one of the most important parameters of a drug-delivery system, and it can be assessed by in vitro, in vivo, and ex vivo methods. The mucin–particle interaction test is an in vitro evaluation method, which basically measures particle size changes after the mucoadhesive IDD system is incubated with mucin [34,35]. The increase in size reflects the interaction between mucin and the system, indicating bioadhesiveness. Similar to the mucin–particle method, another in vitro assessment tool measures the volume of a biological fluid required to wash-out 50% of the mucoadhesive material from a substrate [22,36]. This method compares the retention efficiency of the formulations on mucosal surfaces. In another suggested method, the mucoadhesion capability was measured using a texture analyzer [37,38]; the probe holding the mucosa was kept in contact with the surface of the gel with a contact force of 0.05 N for 2 min, and the probe was subsequently removed vertically upwards at a constant speed of 0.1 mm/s. The maximum detachment force and the area under the curve were determined from the resultant force–distance graph to calculate the work of mucoadhesion. Kaldybekov et al. proposed the mucus incubation method to evaluate the mucoadhesion/retention capability; here, a fluorescent-labeled IDD system is placed on the mucosal side of an excised porcine bladder tissue and then constantly irrigated with artificial urine using a peristaltic pump at a flow rate of 2 mL/min to observe the wash-out process of the formulation using fluorescent images [39].