Formulations and evaluation of Cyclodextrin complexed Ceadroxil loaded nanosponges

Abstract

<p>Cefadroxil (CFD) is a broad spectrum antibiotic that acts against an extensive variety of bacteria, including Gram-positive and Gram-negative bacteria. The major drawback of orally administered drug like cefadroxil is its shorter half life of 1.2 hrs. The goal of the study is to prolong the drug release, producing a desired blood serum level, reduction in drug toxicity and improving the patient compliance by prolonging the dosing intervals. Cyclodextrin-based nanosponges (NS) are a novel class of cross-linked derivatives of cyclodextrins. They have been used to increase the solubility of poorly soluble actives, to protect the labile groups and control the release. This study aimed at formulating complexes of CFDwith three types of β-cyclodextrin NS obtained with different cross-linking ratio (viz. 1:2, 1:4 and 1:8 on molar basis with the cross-linker) to protect the lactone ring from hydrolysis and to prolong the release kinetics of CFD. Crystalline (F<sub>1:2</sub>, F<sub>1:4</sub> and F<sub>1:8</sub>) and paracrystalline NS formulations were prepared. XRPD, DSC and FTIR studies confirmed the interactions of CFDwith NS. XRPD showed that the crystallinity of CFD decreased after loading. CFD was loaded as much as 21%, 37% and 13% w/w in F<sub>1:2 </sub>, F<sub>1:4</sub> and F<sub>1:8</sub>, respectively while the paracrystalline NS formulations gave a loading of about 10% w/w or lower. The particle sizes of the loaded NS formulations were between 450 and 600 nm with low polydispersity indices. The zeta potentials were sufficiently high (-20 to -25 mV) to obtain a stable colloidal nanosuspension. The in vitro studies indicated a slow and prolonged CFD release over a period of 24 h. The NS formulations protected the lactone ring of CFD after their incubation in physiological conditions at 37°C for 24 h with a 80% w/w of intact lactone ring when compared to only around 20% w/w of plain CFD.</p>

Formulation and Evaluation of Ibrutinib Nanosponges Incoporated Tablet

“…The sample was shadowed in a cathodic evaporator with a gold layer 20 nm thick. Photographs were elaborated by an image processing program and individual NP diameters were measured to obtain mean particle size [18].…”

The ascension of nanosponges as a drug delivery carrier: preparation, characterization, and applications

“…The melting point should be below 250 °C and the solubility should be below 10 mg/ml in water [ 65 ]. The compounds with a high melting point have a lower stability constant value after entrapping in NSs and hence, uneven complexes are found between drug and NSs [ 67 ]. Also, the drugs with a high melting will be less entrapped and thus affect the drug loading capacity.…”

Cyclodextrin Inclusion Complexes with Antibiotics and Antibacterial Agents as Drug-Delivery Systems—A Pharmaceutical Perspective

“…A new approach of cefadroxil /β-CD-based nanosponges (NSs) with diphenylcarbonate for the cross-linking was developed to prevent hydrolysis of the lactone ring and prolong the drug release to achieve the desired serum level [ 65 ]. XRPD, DSC, and FT-IR methods confirmed the interactions of cefadroxil with the NS, while in vitro studies showed a sustained release over 24 h.…”