Temperature-Sensitive Gels for Intratumoral Delivery ofβ-Lapachone: Effect of Cyclodextrins and Ethanol

Abstract

This work evaluated the potential of Pluronics (varieties F127 and P123) in combination with solubilizing agents to be used as syringeable in situ gelling depots of intratumoral β-lapachone (βLAP). Pluronic dispersions prepared at various concentrations in the absence and the presence of ethanol and randomly methylated β-cyclodextrin (RMβCD) were characterized regarding their rheological properties, drug solubilization capacity, and in vitro release. Pluronic F127 (18–23%) formulations combined high ability to solubilize βLAP (enhancement solubility factor up to 50), adequate gel temperature range (over 25°C), and gel strength at 37°C enough to guarantee the permanence of the formulation in the administration site for a period of time. βLAP release rate was finely tuned by the concentration of the polymer and the addition of RMβCD (diffusion coefficient ranging between 9 and 69 μg·cm−2). The ethanol increases βLAP release rate but simultaneously led to weak gels. This paper shows that βLAP formulations involving temperature-reversible Pluronic gels may be suitable for intratumoral drug delivery purposes.

Hot melt extruded transdermal films based on amorphous solid dispersions in Eudragit RS PO: The inclusion of hydrophilic additives to develop moisture-activated release systems

“…Pluronic® F127 or poloxamer 407 and Gelucire 44/14 were also used as amphiphilic excipients that can act as solubilising agents. Pluronic® F127 is a non-ionic tri-block copolymer of polyoxyethylene(PEO)-polyoxypropylene(PPO)-polyoxyethylene (PEO) [24] with an HLB value of 22 [25]; this material is considered to be non-irritant and non-sensitising in topical and transdermal applications [26][27]. Gelucire® 44/14, with HLB value of 14, is a mixture of monoesters, diesters and triesters of glycerol, and monoesters and diesters of polyethylene glycols [28] that belongs to the lauryl polyoxylglycerides (macroglycerides) family.…”

Development of In-Situ Spray for Local Delivery of Antibacterial Drug for Hidradenitis Suppurativa: Investigation of Alternative Formulation

“…From the results obtained, the average gelation temperature and gelation time decrease as the concentration of Pluronic F-127 increases, which leads to higher concentration of PPO responsible for the gelation effect. Based on the literation, lower Pluronic F-127 concentration can form a gel at a longer time; however, a concentration above 22% of Pluronic F-127 becomes gel at room temperature that is not considerable for spray formulation [ 32 , 33 ]. The requirement for the gelation temperature of the base formulation was set between 29 °C and 35 °C, and the gelation time was set at less than 2.30 min.…”

Pre-Clinical Assessment of the Nose-to-Brain Delivery of Zonisamide After Intranasal Administration

“…Although drug administration into the nose is often performed using a pipette or a polyethylene tube attached to a microsyringe/micropipette (41,42), herein we preferred to use the MicroSprayer ® Aerosolizer and to load zonisamide in an in situ-gelling hydrogel, the Pluronic F-127 vehicle. This choice was based on our recent studies that demonstrated that almost 50% of levetiracetam undergoes direct nose-tobrain delivery after its nasal administration (23,(41)(42)(43)(44)(45). Nonetheless, to increase in situ-gelling properties and m u c o a d h e s i o n , C a r b o p o l ® 9 7 4 P a n d N o v e o n ® Polycarbophil polymers were herein investigated and subjected to cellular viability tests to select the safest one for IN administration to mice.…”