The Formulation and Evaluation of Topical Berberine-Hydrochloride Products - Pharmaceutical Technology

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The Formulation and Evaluation of Topical Berberine-Hydrochloride Products
The authors sought to prepare a topical formulation of berberine hydrochloride for the effective and controlled management of inflammation and skin infections.

Pharmaceutical Technology
Volume 34, Issue 1, pp. 60-69

The interaction coefficient values indicated the effects of the variables in combination (see Table II). The authors had difficulty ranking the interaction effects, although the strongest interactions appeared to be between T and C. T–C interaction also suggest that S. aureus is more susceptible to cream formulations that contain a high concentration of Apifil than is C. albicans. More importantly, the various interactions appeared to be generally weak, suggesting that the variables were, to a large extent, acting independently of each other. This observation therefore implies that T is the most influential variable in this particular work because it had the largest effects.

Figure 2
In vitro skin-permeation studies. The authors investigated the penetration-enhancing effect of menthol on the permeability of cream formulations of BRB through the excised rat epidermis. Permeation parameters for BRB in the cream formulations are shown in Table III. The cumulative amount of drug permeation through the rat epidermis from cream formulations that contained various amounts of menthol is shown in Figure 2.

The maximum amount (Q 24 ) of BRB that permeated during the 24 h of the study was 6.20 0.23 mg/cm-2 from Formulation P prepared without menthol. The flux was obtained by dividing the cumulative amount of drug permeated per cm2 of the skin by time. The corresponding flux of BRB was 260.21 9.76 μg/cm-2/hr-1 for Formulation P.

Table III: Drug content, viscosity, amount of drug permeated in 24 h (Q24), % BRB released, flux (J), permeability coefficient (Kp), enhancement ratio (ER), and zero-order R2 values for the in vitro permeation study across rat epidermal membrane from cream formulations of BRB containing selected concentrations of menthol at the end of 24 h.
The authors observed a marked effect of menthol on BRB skin permeation. The cumulative amounts (Q 24 ) of BRB that permeated over 24 h increased from 9.43 0.34 to 35.07 0.95 mg cm-2 for cream formulations containing 2.5 and 12.5 %w/w of menthol, respectively. The corresponding flux values ranged from 391.73 12.58 to 1485.75 42.93 μg cm-2 /h-1 . However, a lag period of 1 h was observed for both formulations. The drug-permeation data were consistent with zero-order kinetics from 2 to 24 h with a lag period of about 1 h for all cream formulations (see Table III).

As the menthol concentration increased from 0 to 12.5% w/w, the permeability of BRB also increased, as indicated by an increase in both the permeability coefficient and enhancement ration (ER) (see Figure 2 and Table III). The authors observed a fivefold increase in the permeability of the drug from the cream containing 12.5% w/w of menthol (see Table III). Terpenes increase the drug's percutaneous permeation mainly by disrupting the intercellular packing of the subcutaneous lipids (18–20).


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