The purpose of the study was to develop an SNEDDS to improve the solubility and bioavailability of pitavastatin. The solubility of pitavastatin in different oils, surfactants, and co-surfactants was determined and a pseudo-ternary phase diagram was constructed. The SNEDDS was characterized by zeta-sizer, zeta-potential, FTIR, DSC, and TGA. Release and permeation of pitavastatin from the SNEDDS was studied for 12 and 24 h, respectively. The lipolysis test, RBC lysis, effect on lipid profile, and pharmacokinetics were studied. The SPC3 formulation showed a 104 ± 1.50 nm particle size, a 0.198 polydispersity index (PDI), and a –29 zeta potential. FTIR, DSC, and TGA showed the chemical compatibility and thermal stability. The release and permeation of pitavastatin from SPC3 was 88.5 ± 2.5% and 96%, respectively. In the lipolysis test, the digestion of SPC3 yielded a high amount of pitavastatin and showed little RBC lysis. The lipid profile suggested that after 35 days of administration of the SNEDDS, there was a marked decrease in TC, LDL, and triglyceride levels. The SNEDDS of SPC3 showed an 86% viability of Caco-2 cells. Pharmacokinetics of SPC3 showed improved values of C_max, T_max, half-life, MRT, AUC, and AUMC compared to the reference formulation. Our study demonstrated that the SNEDDS effectively enhanced the solubility and bioavailability of a BCS class II drug.

The development and optimization of controlled release lipospheres (LS) from safe biocompatible behenic acid (BA) was performed for not only enhancing patient’s compliance against highly prevailed chronic diabetes but also to vanquish the insufficiencies of traditional methods of drug delivery. The Box‐Bhenken design (BBD) was utilized to statistically investigate the impact of formulation variables on percentage yield (Y₁), entrapment efficiency (Y₂), and SG‐release (Y₃) from saxagliptin‐ (SG‐) loaded LS, and the chosen optimized LS were subjected to a comparative in vivo pharmacokinetic analysis against commercially available SG brand. The compatibility analysis performed by DSC and FTIR established a complete lack of interaction of formulation components with SG, while p‐XRD suggested a mild transformation of crystalline drug to its amorphous form during encapsulation process. The spherical, free flowing smooth surface LS having zeta potential of ‐32 mV and size range of 11‐20 μm were conveniently formulated. The obtained data for Y₁ (30‐80%), Y₂ (30‐70%), and Y₃ (40‐90%) showed a best fit with quadratic model. The pharmacokinetics analysis of LS showed a significantly decreased C_max of SG (75.63 ± 3.85) with a sufficiently elevated T_max (10.53 h) as compared to commercial brand of SG (99.66 ± 2.97 ng/mL and 3.55 ± 2.18 h). The achievement of greater bioavailability of SG was most probably attributed to higher level of half‐life, mean residence time (MRT), and AUC_0-24 for SG released from LS. Conclusively, the novel approach of SG‐loaded LS had successfully sustained the plasma SG level for a prolonged time without increasing C_max which would ultimately bring an effective management of chronic diabetes.

In the current study, nitrofurazone- (NFZ) and lidocaine-loaded (LD) silica microspheres were fabricated to address pathological indications of skin infections. The microspheres were prepared by the sol–gel method applying the Box–Behnken design and evaluated for size distribution, morphology, zeta potential, physico-chemical compatibility, XRD, thermogravimetric analysis, antibacterial and cytotoxicity activities. The comparative in vitro drug release study of microspheres revealed a 30% release of NFZ and 33% of LD after 8 h. The microspheres showed 81% percentage yield (PY) and 71.9% entrapment efficiency. XRD patterns confirmed the entrapment of NFZ–LD in silica microspheres with a significant reduction in crystallinity of the drugs. Thermal and FTIR studies proved the absence of any profound interactions of the formulation ingredients. The smooth spherical microspheres had a −28 mV zeta potential and a 10–100 µm size distribution. In vitro antibacterial activities of the NFZ–LD microspheres showed an increased zone of inhibition compared to pure drug suspensions. The in vivo efficacy tested on rabbits showed a comparatively rapid wound healing with complete lack of skin irritation impact. The cytotoxicity studies revealed more acceptability of silica microspheres with negligible harm to cells. The study suggests that the NFZ- and LD-loaded silica microspheres would be an ideal system for accelerating and promoting rapid healing of various acute and chronic wounds.

The current study focused on the fabrication of a well-designed, biocompatible, physically stable, non-irritating and highly porous gelatin scaffold loaded with controlled-release triamcinolone acetonide (TA) and econazole nitrate (EN) co-loaded into mesoporous silica nanoparticles (EN-TA-loaded MSNs) to provide a better long-lasting antifungal therapeutic effect with minimal unfavorable effects. Optimization of the MSNs-loaded scaffold was performed using central composite rotatable design (CCRD), where the effect of gelatin concentration (X1), plasticizer (X2) and freezing time (X3) on the entrapment of EN (Y1) and TA (Y2) and on the release of EN (Y3) and TA (Y4) from the scaffold were studied. The significant compatibility of all formulation ingredients with both drugs was established from XRD, DSC and FT-IR spectra analyses while SEM and zeta studies represented a very precise unvarying distribution of the loaded MSNs in the porous structure of the scaffold. The stability of the optimized scaffold was confirmed from zeta potential analysis (−16.20 mV), and it exhibited higher entrapment efficiency (94%) and the slower (34%) release of both drugs. During in vitro and in vivo antifungal studies against Candida albicans, the MSNs-loaded scaffold was comparatively superior in the eradication of fungal infections as a greater zone of inhibition was observed for the optimized scaffold (16.91 mm) as compared to the pure drugs suspension (14.10 mm). Similarly, the MSNs-loaded scaffold showed a decreased cytotoxicity because the cell survival rate in the scaffold presence was 89% while the cell survival rate was 85% in the case of the pure drugs, and the MSNs-loaded scaffold did not indicate any grade of erythema on the skin in comparison to the pure medicinal agents. Conclusively, the scaffold-loaded nanoparticles containing the combined therapy appear to possess a strong prospective for enhancing patients’ adherence and therapy tolerance by yielding improved synergistic antifungal efficacy at a low dose with abridged toxicity and augmented wound-healing impact.

Objectives: To evaluate drug prescribing practices at Medical Unit, ICU and Nephrology Unit, using WHO prescribing indicators, in order to promote rational drug use. Study Design: A retrospective cross sectional study. Place and Duration of Study: Bolan Medical Complex Hospital Quetta, Pakistan, from July to December 2015. Methodology: Drug prescribing trends in 218 prescriptions were scrutinized thoroughly. Data was collected by well-trained pharmacy personals by using prescriptions and prescription registration books of patients. Descriptive statistics were calculated on SPSS version 16.0. Results: The average number of drugs prescribed per prescription were 4.11 whereas, WHO recommends that it should be 2.00 or less. Alternatively, percentage of drugs prescribed by generic name and from an essential drug list were 14.73% and 78.35% while, in accordance with WHO it must be 100% and 70% correspondingly. On the other hand, percentage of encounters having antibiotics or injections prescribed were 18.33% and 32.79% but according to WHO it should be20% or less and 10%respectively. Nevertheless, proper diagnosis was stated in 89.44% of prescriptions and 72.11% prescriptions had complete relevance between treatment and diagnosis. Along with, appropriate drug dosage and their administration was instituted in 65.16% of prescriptions and 73.21% of prescriptions had accurate duration of therapy. Conclusion: The prescribing patterns in Bolan Medical Complex Hospital Quetta reflect the practice of polypharmacy, which is more of an irrational type in contrast to WHO recommendations. Thus, there is an urge to bring about some interventions to improve the pharmacotherapy.