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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
Saxena et al. formulated the pH-sensitive hydrogels of levofloxacin hemihydrates for ophthalmic drug delivery. Levofloxacin is used for the treatment of acute conjunctivitis. β-cyclodextrin were added in addition to the polymers Carbopol 940 and HPMC, to increase the solubility of levofloxacin. Ocular irritation studies in albino rabbits showed that the formulation does not cause damage to the cornea, iris, and conjunctiva [117].
Nanocarrier Technologies for Enhancing the Solubility and Dissolution Rate of Api
Published in Debarshi Kar Mahapatra, Sanjay Kumar Bharti, Medicinal Chemistry with Pharmaceutical Product Development, 2019
Ashwini Deshpande, Tulshidas S. Patil
Oridonin (Odn)–2 hydroxypropyl-β-cyclodextrin inclusion complexes (Odn-CICs) containing nanosuspensions were developed by solvent evaporation followed by wet media milling technique. Significant improvement in dissolution of oridonin through Odn-CICs was observed. Marked improvement in the intestinal effective permeability of drug was noticed in the presence of 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) and poloxamer. Odn-nanosuspension demonstrated significantly increased in oral absorption with a relative bioavailability of 213.99% [162].
Gas Chromatography
Published in Joseph Chamberlain, The Analysis of Drugs in Biological Fluids, 2018
The diamide phases belong to the class of separations dependent on the three- point attachment hypothesis covered more fully in Chapter 7 on liquid chromatography. Cyclodextrins are cyclic glucose oligomers with 6 (α-cyclodextrin), 7 (β cyclodextrin) or 8 (γ-cyclodextrin) linked glucose units, and separate compounds by size inclusion of molecules in the cavity formed by the cyclic molecule and the chiral property arises from the unique topology formed by the chirality of the glucose units (Figure 6.6). The stability and selectivity of cyclodextrins has been improved by formation of suitable alkyl and acyl derivatives640,641,644 and by combination with siloxanes.642
New chromatographic insights on drug:cyclodextrin inclusion complexes and their potential use in drug delivery
Published in Expert Opinion on Drug Delivery, 2022
Marieta Constantin, Bogdan Cosman, Paolo Ascenzi, Bogdan C. Simionescu, Gheorghe Fundueanu
Here, Pul/β-CD and Pul/HP-β-CD microgels were prepared by suspension cross-linking of the pullulan:CD mixture. Microgels containing equivalent amounts of β-CD and HP-β-CD were packed in a chromatographic column, and the retention time of several drugs and model compounds was determined. Drugs and model compounds were classified according to their retention times; chemicals with the longest retention times (eugenol, methyl-paraben, ethyl-paraben, and ibuprofen) were considered to form the strongest inclusion complexes. Then these compounds were included in Pul/CD microgels, and the kinetics of their release was investigated under simulated physiological conditions. As a result of these investigations, it was answered three major questions: Can cyclodextrins that form strong inclusion complexes sustain a prolonged release of drugs? How fast are the formation and cleavage of drug:cyclodextrin complexes? Does β-cyclodextrin form more stable inclusion complexes than hydroxypropyl-β-cyclodextrin?
In vitro and in vivo characteristics of doxorubicin-loaded cyclodextrine-based polyester modified gadolinium oxide nanoparticles: a versatile targeted theranostic system for tumour chemotherapy and molecular resonance imaging
Published in Journal of Drug Targeting, 2020
Tohid Mortezazadeh, Elham Gholibegloo, Mehdi Khoobi, Nader Riyahi Alam, Soheila Haghgoo, Asghar Mesbahi
β-Cyclodextrin (β-CD) is a cyclic oligosaccharide, having the hydrophilic outer surface and lipophilic central cavity. The hydrophobic cavity of β-CD can serve for reversible host-guest interaction with different poorly water-soluble and size-matched molecules, thereby improving the solubility, bioavailability and safety of hydrophobic drugs [7,8]. The binding strength of the inclusion complexes mainly depends on conformational energy gain, hydrophobic interactions and hydrogen bonds. Myriad primary hydroxyl groups in upper rim and secondary hydroxyls in the lower rim of the exterior surface provide a valuable opportunity for selective modification of β-CD with various functional moieties imparting the system with tailored functionalities [9]. Also, β-CD can employ for pH-reversible host–guest interaction with hydrophobic cargo bearing protonable groups making this cyclic oligosaccharide as best candidate for selective delivery of anticancer agents at tumour sites. Hydrophobic anticancer agents can be protonated at tumour sites (pH 6.5–6.8 for extracellular and <6.0 for intracellular matrix) and converted to the hydrophilic ionic salt resulting in the much faster release of the drug from hydrophobic cavity of CD [10].
β-Sitosterol-loaded solid lipid nanoparticles ameliorate complete Freund’s adjuvant-induced arthritis in rats: involvement of NF-кB and HO-1/Nrf-2 pathway
Published in Drug Delivery, 2020
Feng Zhang, Zhiyu Liu, Xijing He, Zhanqi Li, Bin Shi, Fengmei Cai
As my knowledge, few of the studies have been carried out on the β-sitosterol to improve the therapeutic efficacy. Most of the investigations conducted with β-sitosterol have focused on using it and its derivatives as an excipients to regulate drug release or promote drug absorption (Farkas et al., 2006; Lacatusu et al., 2012). In previous study, cyclodextrins has been used to increase the aqueous bioavailability and solubility of β-sitosterol. Imanaka et al., showed that the liposomal containing formulation of β-sitosterol enhanced the natural killer cell activity and reduced the B16BL6 melanoma cells colonies in the lungs of experimental mice (Imanaka et al., 2008). Awad et al., showed the protective effect of β-sitosterol against various cancer cells via involving the 2-hydroxypropyl-β-cyclodextrin (HP-βCD) as a carrier vehicle (Awad et al., 2000, 2001, 2007). These investigations showed that β-sitosterol reduced the cell proliferation after the 3–5 days at 16–32 µM. It is well documented that cyclodestrins commonly used in the pharmaceutical preparations as excipients to increase the bioavailability and solubility. We hypothesized that solid lipid nano-particles of β-sitosterol can offer better enhancement of antiarthritic effect against the rodent model. This assumption is due to various beneficial effect of SLN such as improved drug-loading capacity, controlled release, facilitated, improved solubility and targeted drug release.