Home
Resources
Publications
In Vitro and Ex Vivo Studies on Diltiazem Hydrochloride-Loaded Microsponges in Rectal Gels for Chronic Anal Fissures Treatment

In Vitro and Ex Vivo Studies on Diltiazem Hydrochloride-Loaded Microsponges in Rectal Gels for Chronic Anal Fissures Treatment

Nadezhda Antonova Ivanova, Adriana Trapani, Cinzia Di Franco, Delia Mandracchia, Giuseppe Trapani, Carlo Franchini, Filomena Corbo, Giuseppe Tripodo, Iliyan Nikolov Kolev, Georgi Stoyanov Stoyanov, Kameliya Zhechkova Bratoeva

Int J Pharm. 2019 Feb 25;557:53-65.

PMID: 30580086

Abstract:

Diltiazem hydrochloride, topically applied at 2% concentration, is considered effective for the treatment of chronic anal fissures, although it involves several side effects among which anal pruritus and postural hypotension. To test the hypothesis that a sustained delivery system of diltiazem hydrochloride may be helpful for the treatment of chronic anal fissures, in the present study we evaluated the potential of gels containing diltiazem hydrochloride entrapped in microsponges. Such microsponges were based on Eudragit RS 100 and the effect of some formulation variables was assessed by a 23 full factorial screening design. An optimized formulation of diltiazem hydrochloride microsponges was dispersed in Methylcellulose 2% or Poloxamer 407 20% and the resulting gels (micro-l-diltiazem hydrochloride 2%) were subjected to in vitro drug release, ex vivo permeability and drug deposition after application on porcine rectal mucosa. The results showed a prolonged release up to 24 h from micro-l-diltiazem hydrochloride at 2% in the gels. The permeation tests revealed up to 18% higher drug retention on the mucosal tissue after 24 h by the micro-l-diltiazem hydrochloride 2% gels compared to conventional diltiazem hydrochloride gels at 2%. These results suggest that diltiazem hydrochloride-loaded microsponges dispersed in rectal gels may be useful to overcome some limitations of conventional local chronic anal fissure therapy.

Chemicals Related in the Paper:

Catalog Number	Product Name	CAS Number	Price
ALP853220527	CID 11210285 hydrochloride	853220-52-7 (free base)	Price
AP115918600	L-Serine-7-amido-4-methylcoumarin hydrochloride	115918-60-0	Price
AP2179159	Z-L-Lys-ONp hydrochloride	2179-15-9	Price
IAR42410163	L-Arginine-15N4 hydrochloride		Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: