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Preparation of Tamsulosin Hydrochloride-Loaded Mucoadhesive In Situ Gelling Polymeric Formulation for Nasal Delivery in Geriatrics
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Preparation of Tamsulosin Hydrochloride-Loaded Mucoadhesive In Situ Gelling Polymeric Formulation for Nasal Delivery in Geriatrics
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Preparation of Tamsulosin Hydrochloride-Loaded Mucoadhesive In Situ Gelling Polymeric Formulation for Nasal Delivery in Geriatrics
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Journal Article
Preparation of Tamsulosin Hydrochloride-Loaded Mucoadhesive In Situ Gelling Polymeric Formulation for Nasal Delivery in Geriatrics
2023
نظرة عامة
This study aimed to prepare tamsulosin hydrochloride (HCl)-loaded
in situ
gelling formulation by using hydroxypropyl methylcellulose (HPMC), gellan gum, poloxamer 188, and benzalkonium chloride. Physicochemical evaluation of formulations included determination of pH, viscosity, gelation time, gel strength, drug content, and sterility.
In silico
study was performed to analyze interactions between polymers, drug, and mucin glycoprotein.
In vitro
degradation time, drug release,
ex vivo
mucoadhesion time, permeation,
in vivo
pharmacokinetics, and stability studies were performed to assess the formulation. Formulations were transparent and displayed acceptable physicochemical attributes. Tamsulosin HCl and polymers interacted via non-covalent interactions. HPMC formed hydrogen bonds, hydrophobic and
van der Waals
interactions with mucin protein while the drug formed hydrogen bonds only. Gel formulation degraded in simulated nasal fluid within 24 h.
In situ
gelling formulation showed 83.8 ± 1.7% drug release and remained adhered to the mucosa for 24.5 ± 1 h. A higher (~ 1.85 times) drug permeation was recorded through mucosa within 6 h by
in situ
gelling formulation when compared to control counterparts (aqueous solution of drug and
in situ
gelling formulation without poloxamer 188). Nasal administration of tamsulosin HCl by using
in situ
gelling formulation led to a ~ 3.3 and ~ 3.5 times, respectively, higher Cmax (maximum plasma concentration) and AUC
total
(total area under the curve) than the orally administered aqueous solution. Relative bioavailability of drug delivered by nasal
in situ
gelling formulation was 3.5 times the oral counterpart. These results indicated that the prepared
in situ
gelling formulation can act as a promising candidate for systemic administration of tamsulosin HCl.
Graphical Abstract
الناشر
Springer International Publishing
موضوع
