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    • In this analysis the optimized formulation A

    2018-10-22

    In this analysis, the optimized formulation A) F3, B) Guggul lipid, C) Phenylbutazone and D) Cholesterol were subjected to controlled temperature program in a controlled atmosphere. The combined TGA graph shown in (Fig. 4), that the TGA graph of pure drug showed that the mass remained constant with increasing temperature but as it Wortmannin approached melting point of drug, the started to fallen down. Similar phenomenon was also observed with the formulated guggulosome F3 which shown a sharp falling of the curve at the 250° C, that reveals that the combination of guggul lipid with the drug enhances its stability. An another TGA study was done for the guggul alone and its shown a sharp falling curve at 140° C. all these findings revealed that excipients or moisture content have no adverse effect on formulations (see Table 1). The entrapment efficiency of drug in guggulosomes is dependent on numerous factors like the ratio of lipid i.e. ratio of guggul lipid and cholesterol and the ratio of dug to total lipid. The entrapment efficiency of the phenylbutazone in the guggulosomes was determined by the centrifugation technique. We observed that with increase in cholesterol concentration and constant amount of drug and different amount of guggul lipid as 100, 200, 300, 400 mg, in the formulations F5-F6, F2- F1 & F3- F4 respectively, the percentage encapsulation efficiency were found to be 58.1 ± 0.84, 68.9 ± 0.21, 68.3 ± 0.56, 73.8 ± 0.282, 77.2 ± 0.212, and 55 ± 0.162. Formulation F3 with highest amount of guggul lipid (400 mg), cholesterol (400 mg) with constant amount of drug showed better & maximum entrapment efficiency. From the result obtained shown in (Table 2). we can say that the an appropriate ratio of guggul and cholesterol conc. play an important role in the entrapment efficiency, this is due to increase in overall lipid conc. that favors the nature of drug to be encapsulate in the core as a whole. The particle size and polydispersity index (PDI) were determined by using dynamic light scattering technique and are show in Table 2. All the formulations, F1- F6 showed mean particle diameter sizes ranging from 230.2  ±  0.14 to 342.3 ± 3.04 nm with PDI ranging between 0.225 ± 0.32 to 0.614 ± 0.27. Formulation F3 containing guggul lipid (400 mg) and cholesterol (400 mg) with the same amount of drug (150 mg) has shown the mean particle size (287.3  ± 1.13), which is an optimum formulation having PDI (0.289  ±  0.23). By the help of above observations we can conclude that particle size of F3 shown in (Fig. 5) was suitable for topical use. The guggulosomal formulations F1 to F6 showed zeta potential value ranging from -20.1to -35.7 mV are shown in (Table 2.). Formulations F5, F6 and F1 with cholesterol concentration 100, 200, and 300 shown zeta potential −20.1, −21.2 and −25.9 mV respectively while with the highest concentration of cholesterol 200, 300, and 400 in formulations F2, F4, and F3 showed an increase in zeta potential of value −26.5, −29.8 and −35.7 respectively. These finding reveals that upon increasing the cholesterol concentration, the surface charge (negative) on the guggulosomes increases and thus lead to be increased in the stability. This result clearly shown that the formulation F3 is the most stable formulation prepared by trituration method and has shown in (Fig. 5). The in-vitro release of all formulations loaded with phenylbutazone was studied. The drug release from guggulosomes was formulated by use of various concentrations of guggul lipid, cholesterol and phenylbutazone. The in vitro release studies of F1 to F6 formulations were studied and the results of the same were showed in (Fig. 6) The formulations F1 to F6 have shown the following drug release 37.50 ± 0.1.40, 55.48 ± 0.1.41, 60.80 ± 0.707, 44.03 ± 0.1.40, 44.21 ± 1.41, and 46.53 ± 0.707, after 24 h respectively. Formulation F3 prepared by trituration method show maximum percent cumulative drug release profile due to high loading of drug in guggulosomes in comparison to other formulation. 60.80 ± 0.707% phenylbutazone release from guggulosomes showed drug release for 24hr and burst release in initially 8hr and gradually release decreases and becomes constant in 18 h. The drug release was sustained due to addition of cholesterol in formulation to provide rigidity to the lipid vesicles of phenylbutazone. Thus cholesterol and guggul lipid acts as rate-limiting membrane for release of the phenylbutazone loaded guggulosomes. Formulation F1 showed minimum release of phenylbutazone due to increase in amount of cholesterol which increases the rigidity of guggulosomes vesicles. The results depicted that variation in guggul lipid and cholesterol concentration may affect the drug release pattern which is also mention by (Jithan AV et al, l; 2010) [25].