Enhanced dissolution and stability of Tanshinone IIA base by solid dispersion system with nano-hydroxyapatite

Abstract

Background:Tanshinone IIA (TSIIA) exhibits a variety of cardiovascular effects; however, it has low solubility in water. The preparation of poorly soluble drugs for oral delivery is one of the greatest challenges in the field of formulation research. Among the approaches available, solid dispersion (SD) technique has proven to be one of the most commonly used these methods for improving dissolution and bioavailability of drugs, because of its relative simplicity and economy in terms of both preparation and evaluation.Objective:This study was aimed at investigating the dissolution behavior and physical stability of SDs of TSIIA by employing nano-hydroxyapatite (n-HAp).Materials and Methods:The TSIIA SDs was prepared to use a spray-drying method. First, an in vitro dissolution test was performed to assess dissolution characteristics. Next, a set of complementary techniques (differential scanning calorimetry, scanning electron microscopy, X-ray powder diffraction, and Fourier transform infrared spectroscopy) was used to monitor the physicochemical properties of the SDs. The SDs was stored at 40°C/75% relative humidity for 6 months, after which their stability was assessed.Results:TSIIA dissolution remarkably improved because of the formulation of the SDs with n-HAp particles. Comparisons with the corresponding physical mixtures revealed changes in the SDs and explained the formation of the amorphous phase. In the stability test, virtually no time-dependent decrease was observed in either in vitro drug dissolution or drug content.Conclusion:SD formulation with n-HAp may be a promising approach for enhancing the dissolution and stability of TSIIA.

Discovery and Current Status of Evaluation System of Bioavailability and Related Pharmaceutical Technologies for Traditional Chinese Medicines—Flos Lonicerae Japonicae—Fructus Forsythiae Herb Couples as an Example

“…However, formulation designation and pharmaceutical technology applications are severely disrupted by the complex physico-chemical properties for both active ingredients and their associated constituents in TCMs. As reported in the PubMed Database (2006–current), the pharmaceutical methods applied to TCMs classified II (high permeability and low solubility) in the Biopharmaceutics Classification System (BCS) [ 76 ] included mainly micronization [ 77 , 78 ], nano-suspensions [ 79 , 80 , 81 , 82 , 83 , 84 , 85 , 86 , 87 , 88 , 89 , 90 ], solid dispersion [ 91 , 92 , 93 , 94 , 95 , 96 , 97 , 98 , 99 , 100 , 101 , 102 , 103 , 104 , 105 , 106 , 107 , 108 ], phospholipid complex [ 92 , 109 , 110 , 111 , 112 , 113 , 114 , 115 , 116 , 117 , 118 , 119 , 120 ], β-cyclodextrin complex [ 121 , 122 , 123 , 124 , 125 , 126 ,…”

Biotinylated-lipid bilayer coated mesoporous silica nanoparticles for improving the bioavailability and anti-leukaemia activity of Tanshinone IIA

“…However, TanIIA is a typical biopharmaceutical classification system (BCS) Class II drug with a high Log p value (3.1) and a poor water solubility (2.8 ngÁml À1 ) [3,4]. Various approaches such as solid dispersion technologies and the use of colloidal carriers have been adopted to improve the solubility of TanIIA [5][6][7]. Recently, mesoporous materials, classified as having pore diameters in the range from 2 to 50 nm by the International Union of Pure and Applied Chemistry (IUPAC) nomenclature, have been investigated as a vehicle to improve the oral bioavailability of poorly water-soluble drugs [8,9].…”

Traditional and Novel Methods for Cocrystal Formation: A Mini Review

“…5 For example, solid dispersion successfully forms to improve dissolution of Andrographolide, a natural antibiotic 6 and Tanshinone IIA, a cardiovascular agent. 7 Recently, a newer solid state modification, namely pharmaceutical cocrystal gain a high popularity because of its feasibility compared to other methods. Pharmaceutical cocrystal defined as a solid modification of drugs, consists of drug and coformer at stoichiometry ratio that connected by non-covalent interaction, mostly through hydrogen bonding, and can be used to alter physical properties of a drug, especially a drug's solubility without altering its pharmacology effect.…”